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BI 2536 inhibiteur de PLK1/BRD4

Name: BI 2536
Brand: Selleck Chemicals
SKU: S1109
Rating: 5 (299 reviews)

N° Cat.S1109

BI-2536 est un puissant inhibiteur de Plk1 avec une IC50 de 0,83 nM dans un test sans cellules. BI-2536 inhibe Bromodomain 4 (BRD4) avec un Kd de 37 nM et supprime puissamment l'expression de c-Myc. BI-2536 induit Apoptosis et atténue Autophagy. Phase 2.

BI 2536 PLK inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 521.66

Aller à

Contrôle qualité

Lot : Pureté : 99.88%

99.88

Cibles apparentées	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
Autre PLK Inhibiteurs	Volasertib (BI6727) Rigosertib (ON-01910) GSK461364 Onvansertib (NMS-1286937, NMS-P937) CFI-400945 HMN-214 Ro3280 SBE 13 HCl MLN0905 Centrinone (LCR-263)

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	PMID
PSN1	Growth Inhibition Assay				IC50=0.00776 μM	SANGER
ACN	Growth Inhibition Assay				IC50=0.00843 μM	SANGER
TE-8	Growth Inhibition Assay				IC50=0.00941 μM	SANGER
LC-2-ad	Growth Inhibition Assay				IC50=0.01093 μM	SANGER
ALL-PO	Growth Inhibition Assay				IC50=0.013 μM	SANGER
EW-16	Growth Inhibition Assay				IC50=0.01336 μM	SANGER
KM12	Growth Inhibition Assay				IC50=0.01348 μM	SANGER
GI-1	Growth Inhibition Assay				IC50=0.01383 μM	SANGER
LS-411N	Growth Inhibition Assay				IC50=0.01407 μM	SANGER
ES8	Growth Inhibition Assay				IC50=0.01494 μM	SANGER
SNU-C2B	Growth Inhibition Assay				IC50=0.01526 μM	SANGER
CESS	Growth Inhibition Assay				IC50=0.01602 μM	SANGER
697	Growth Inhibition Assay				IC50=0.01668 μM	SANGER
NCI-H1963	Growth Inhibition Assay				IC50=0.01673 μM	SANGER
IA-LM	Growth Inhibition Assay				IC50=0.01688 μM	SANGER
SW954	Growth Inhibition Assay				IC50=0.01705 μM	SANGER
RL95-2	Growth Inhibition Assay				IC50=0.01738 μM	SANGER
LXF-289	Growth Inhibition Assay				IC50=0.0177 μM	SANGER
OCUB-M	Growth Inhibition Assay				IC50=0.01826 μM	SANGER
RKO	Growth Inhibition Assay				IC50=0.01987 μM	SANGER
LOUCY	Growth Inhibition Assay				IC50=0.0205 μM	SANGER
NOS-1	Growth Inhibition Assay				IC50=0.02093 μM	SANGER
A4-Fuk	Growth Inhibition Assay				IC50=0.02218 μM	SANGER
A388	Growth Inhibition Assay				IC50=0.02227 μM	SANGER
TE-9	Growth Inhibition Assay				IC50=0.02261 μM	SANGER
KURAMOCHI	Growth Inhibition Assay				IC50=0.02285 μM	SANGER
KALS-1	Growth Inhibition Assay				IC50=0.02338 μM	SANGER
HOP-62	Growth Inhibition Assay				IC50=0.0242 μM	SANGER
RPMI-8402	Growth Inhibition Assay				IC50=0.02508 μM	SANGER
TE-1	Growth Inhibition Assay				IC50=0.02512 μM	SANGER
CCRF-CEM	Growth Inhibition Assay				IC50=0.02543 μM	SANGER
HUTU-80	Growth Inhibition Assay				IC50=0.02624 μM	SANGER
NCI-H1648	Growth Inhibition Assay				IC50=0.02647 μM	SANGER
HCE-4	Growth Inhibition Assay				IC50=0.02682 μM	SANGER
ETK-1	Growth Inhibition Assay				IC50=0.02736 μM	SANGER
TE-15	Growth Inhibition Assay				IC50=0.02738 μM	SANGER
BE-13	Growth Inhibition Assay				IC50=0.0274 μM	SANGER
KE-37	Growth Inhibition Assay				IC50=0.02741 μM	SANGER
NCI-H1355	Growth Inhibition Assay				IC50=0.02783 μM	SANGER
TE-11	Growth Inhibition Assay				IC50=0.02809 μM	SANGER
BL-70	Growth Inhibition Assay				IC50=0.02857 μM	SANGER
ES6	Growth Inhibition Assay				IC50=0.02881 μM	SANGER
GT3TKB	Growth Inhibition Assay				IC50=0.02953 μM	SANGER
LB647-SCLC	Growth Inhibition Assay				IC50=0.03195 μM	SANGER
NB13	Growth Inhibition Assay				IC50=0.03316 μM	SANGER
ST486	Growth Inhibition Assay				IC50=0.03337 μM	SANGER
NCI-H82	Growth Inhibition Assay				IC50=0.03343 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay				IC50=0.03399 μM	SANGER
ES4	Growth Inhibition Assay				IC50=0.03463 μM	SANGER
SK-NEP-1	Growth Inhibition Assay				IC50=0.03499 μM	SANGER
Becker	Growth Inhibition Assay				IC50=0.03555 μM	SANGER
A101D	Growth Inhibition Assay				IC50=0.03748 μM	SANGER
SK-UT-1	Growth Inhibition Assay				IC50=0.03774 μM	SANGER
SW982	Growth Inhibition Assay				IC50=0.0379 μM	SANGER
TE-10	Growth Inhibition Assay				IC50=0.04046 μM	SANGER
OVCAR-4	Growth Inhibition Assay				IC50=0.04059 μM	SANGER
KP-N-YS	Growth Inhibition Assay				IC50=0.04085 μM	SANGER
BL-41	Growth Inhibition Assay				IC50=0.04125 μM	SANGER
MZ1-PC	Growth Inhibition Assay				IC50=0.04127 μM	SANGER
PF-382	Growth Inhibition Assay				IC50=0.04198 μM	SANGER
MOLT-13	Growth Inhibition Assay				IC50=0.04238 μM	SANGER
HCC1599	Growth Inhibition Assay				IC50=0.04258 μM	SANGER
IST-MEL1	Growth Inhibition Assay				IC50=0.04442 μM	SANGER
LU-139	Growth Inhibition Assay				IC50=0.04442 μM	SANGER
MS-1	Growth Inhibition Assay				IC50=0.04701 μM	SANGER
MFH-ino	Growth Inhibition Assay				IC50=0.05003 μM	SANGER
IMR-5	Growth Inhibition Assay				IC50=0.05021 μM	SANGER
TE-5	Growth Inhibition Assay				IC50=0.05063 μM	SANGER
DJM-1	Growth Inhibition Assay				IC50=0.05142 μM	SANGER
NB17	Growth Inhibition Assay				IC50=0.05207 μM	SANGER
KARPAS-45	Growth Inhibition Assay				IC50=0.05358 μM	SANGER
TGBC1TKB	Growth Inhibition Assay				IC50=0.05405 μM	SANGER
ML-2	Growth Inhibition Assay				IC50=0.05414 μM	SANGER
no-10	Growth Inhibition Assay				IC50=0.05474 μM	SANGER
CTV-1	Growth Inhibition Assay				IC50=0.05502 μM	SANGER
SJSA-1	Growth Inhibition Assay				IC50=0.0552 μM	SANGER
HC-1	Growth Inhibition Assay				IC50=0.05597 μM	SANGER
TE-12	Growth Inhibition Assay				IC50=0.05613 μM	SANGER
KY821	Growth Inhibition Assay				IC50=0.05632 μM	SANGER
TALL-1	Growth Inhibition Assay				IC50=0.05708 μM	SANGER
DEL	Growth Inhibition Assay				IC50=0.05709 μM	SANGER
TE-6	Growth Inhibition Assay				IC50=0.05722 μM	SANGER
SK-LMS-1	Growth Inhibition Assay				IC50=0.05805 μM	SANGER
EW-1	Growth Inhibition Assay				IC50=0.05837 μM	SANGER
8-MG-BA	Growth Inhibition Assay				IC50=0.05851 μM	SANGER
NALM-6	Growth Inhibition Assay				IC50=0.05973 μM	SANGER
LB771-HNC	Growth Inhibition Assay				IC50=0.05979 μM	SANGER
HT-144	Growth Inhibition Assay				IC50=0.0613 μM	SANGER
KM-H2	Growth Inhibition Assay				IC50=0.06221 μM	SANGER
SF268	Growth Inhibition Assay				IC50=0.06286 μM	SANGER
RS4-11	Growth Inhibition Assay				IC50=0.06304 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay				IC50=0.06319 μM	SANGER
ATN-1	Growth Inhibition Assay				IC50=0.06345 μM	SANGER
BB30-HNC	Growth Inhibition Assay				IC50=0.06436 μM	SANGER
CPC-N	Growth Inhibition Assay				IC50=0.06524 μM	SANGER
NB1	Growth Inhibition Assay				IC50=0.06613 μM	SANGER
KS-1	Growth Inhibition Assay				IC50=0.06748 μM	SANGER
RXF393	Growth Inhibition Assay				IC50=0.06764 μM	SANGER
IST-SL2	Growth Inhibition Assay				IC50=0.07004 μM	SANGER
GI-ME-N	Growth Inhibition Assay				IC50=0.07286 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay				IC50=0.07475 μM	SANGER
NCI-H1581	Growth Inhibition Assay				IC50=0.07478 μM	SANGER
U-266	Growth Inhibition Assay				IC50=0.07497 μM	SANGER
DMS-114	Growth Inhibition Assay				IC50=0.07528 μM	SANGER
NCI-H187	Growth Inhibition Assay				IC50=0.07726 μM	SANGER
SW962	Growth Inhibition Assay				IC50=0.07839 μM	SANGER
MONO-MAC-6	Growth Inhibition Assay				IC50=0.07986 μM	SANGER
MOLT-16	Growth Inhibition Assay				IC50=0.08121 μM	SANGER
KNS-42	Growth Inhibition Assay				IC50=0.08161 μM	SANGER
CMK	Growth Inhibition Assay				IC50=0.08225 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay				IC50=0.08225 μM	SANGER
Daudi	Growth Inhibition Assay				IC50=0.08256 μM	SANGER
NCI-H510A	Growth Inhibition Assay				IC50=0.08336 μM	SANGER
LB831-BLC	Growth Inhibition Assay				IC50=0.08561 μM	SANGER
HEL	Growth Inhibition Assay				IC50=0.08668 μM	SANGER
LU-134-A	Growth Inhibition Assay				IC50=0.08708 μM	SANGER
NCI-H1694	Growth Inhibition Assay				IC50=0.08744 μM	SANGER
KGN	Growth Inhibition Assay				IC50=0.08759 μM	SANGER
A253	Growth Inhibition Assay				IC50=0.08822 μM	SANGER
DG-75	Growth Inhibition Assay				IC50=0.08922 μM	SANGER
MOLT-4	Growth Inhibition Assay				IC50=0.08983 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay				IC50=0.09258 μM	SANGER
ONS-76	Growth Inhibition Assay				IC50=0.09276 μM	SANGER
NCI-H446	Growth Inhibition Assay				IC50=0.09462 μM	SANGER
COR-L279	Growth Inhibition Assay				IC50=0.09556 μM	SANGER
Calu-6	Growth Inhibition Assay				IC50=0.09598 μM	SANGER
BC-3	Growth Inhibition Assay				IC50=0.09662 μM	SANGER
NCI-H2126	Growth Inhibition Assay				IC50=0.09791 μM	SANGER
NCI-H1882	Growth Inhibition Assay				IC50=0.09809 μM	SANGER
BB65-RCC	Growth Inhibition Assay				IC50=0.10294 μM	SANGER
DU-4475	Growth Inhibition Assay				IC50=0.10407 μM	SANGER
NCI-H526	Growth Inhibition Assay				IC50=0.1044 μM	SANGER
NEC8	Growth Inhibition Assay				IC50=0.10525 μM	SANGER
NCI-H1304	Growth Inhibition Assay				IC50=0.10594 μM	SANGER
L-540	Growth Inhibition Assay				IC50=0.10708 μM	SANGER
NCI-SNU-16	Growth Inhibition Assay				IC50=0.10742 μM	SANGER
HD-MY-Z	Growth Inhibition Assay				IC50=0.10856 μM	SANGER
K-562	Growth Inhibition Assay				IC50=0.10858 μM	SANGER
JAR	Growth Inhibition Assay				IC50=0.10925 μM	SANGER
MZ2-MEL	Growth Inhibition Assay				IC50=0.1105 μM	SANGER
L-363	Growth Inhibition Assay				IC50=0.11079 μM	SANGER
BV-173	Growth Inhibition Assay				IC50=0.11243 μM	SANGER
NCI-H524	Growth Inhibition Assay				IC50=0.11274 μM	SANGER
EoL-1-cell	Growth Inhibition Assay				IC50=0.11672 μM	SANGER
K052	Growth Inhibition Assay				IC50=0.11712 μM	SANGER
TK10	Growth Inhibition Assay				IC50=0.11728 μM	SANGER
KU812	Growth Inhibition Assay				IC50=0.12044 μM	SANGER
RPMI-8226	Growth Inhibition Assay				IC50=0.12052 μM	SANGER
MZ7-mel	Growth Inhibition Assay				IC50=0.12237 μM	SANGER
SK-PN-DW	Growth Inhibition Assay				IC50=0.12287 μM	SANGER
SR	Growth Inhibition Assay				IC50=0.12441 μM	SANGER
RPMI-6666	Growth Inhibition Assay				IC50=0.12743 μM	SANGER
no-11	Growth Inhibition Assay				IC50=0.12869 μM	SANGER
EW-3	Growth Inhibition Assay				IC50=0.12893 μM	SANGER
LAMA-84	Growth Inhibition Assay				IC50=0.13187 μM	SANGER
HT	Growth Inhibition Assay				IC50=0.13574 μM	SANGER
KP-N-RT-BM-1	Growth Inhibition Assay				IC50=0.13612 μM	SANGER
NCI-H747	Growth Inhibition Assay				IC50=0.137 μM	SANGER
NCCIT	Growth Inhibition Assay				IC50=0.13939 μM	SANGER
MLMA	Growth Inhibition Assay				IC50=0.14167 μM	SANGER
LP-1	Growth Inhibition Assay				IC50=0.1424 μM	SANGER
CAL-148	Growth Inhibition Assay				IC50=0.14483 μM	SANGER
GB-1	Growth Inhibition Assay				IC50=0.14526 μM	SANGER
COR-L88	Growth Inhibition Assay				IC50=0.14802 μM	SANGER
NKM-1	Growth Inhibition Assay				IC50=0.14906 μM	SANGER
NB5	Growth Inhibition Assay				IC50=0.15462 μM	SANGER
SH-4	Growth Inhibition Assay				IC50=0.15466 μM	SANGER
EM-2	Growth Inhibition Assay				IC50=0.15467 μM	SANGER
TGBC24TKB	Growth Inhibition Assay				IC50=0.15659 μM	SANGER
SCLC-21H	Growth Inhibition Assay				IC50=0.15702 μM	SANGER
COLO-684	Growth Inhibition Assay				IC50=0.15721 μM	SANGER
KINGS-1	Growth Inhibition Assay				IC50=0.1591 μM	SANGER
LS-123	Growth Inhibition Assay				IC50=0.15917 μM	SANGER
MC116	Growth Inhibition Assay				IC50=0.16158 μM	SANGER
SU-DHL-1	Growth Inhibition Assay				IC50=0.16206 μM	SANGER
NCI-H64	Growth Inhibition Assay				IC50=0.16347 μM	SANGER
HCE-T	Growth Inhibition Assay				IC50=0.16504 μM	SANGER
LOXIMVI	Growth Inhibition Assay				IC50=0.16949 μM	SANGER
ARH-77	Growth Inhibition Assay				IC50=0.17379 μM	SANGER
DOHH-2	Growth Inhibition Assay				IC50=0.17672 μM	SANGER
COLO-320-HSR	Growth Inhibition Assay				IC50=0.18154 μM	SANGER
NB6	Growth Inhibition Assay				IC50=0.18566 μM	SANGER
L-428	Growth Inhibition Assay				IC50=0.18813 μM	SANGER
SNB75	Growth Inhibition Assay				IC50=0.18824 μM	SANGER
NCI-H2141	Growth Inhibition Assay				IC50=0.19011 μM	SANGER
KARPAS-299	Growth Inhibition Assay				IC50=0.19241 μM	SANGER
LC4-1	Growth Inhibition Assay				IC50=0.19502 μM	SANGER
UACC-257	Growth Inhibition Assay				IC50=0.19947 μM	SANGER
EVSA-T	Growth Inhibition Assay				IC50=0.20312 μM	SANGER
JiyoyeP-2003	Growth Inhibition Assay				IC50=0.20477 μM	SANGER
NCI-H720	Growth Inhibition Assay				IC50=0.20525 μM	SANGER
GAK	Growth Inhibition Assay				IC50=0.21189 μM	SANGER
HH	Growth Inhibition Assay				IC50=0.21405 μM	SANGER
NCI-H1436	Growth Inhibition Assay				IC50=0.21464 μM	SANGER
GR-ST	Growth Inhibition Assay				IC50=0.21488 μM	SANGER
BC-1	Growth Inhibition Assay				IC50=0.22616 μM	SANGER
SIG-M5	Growth Inhibition Assay				IC50=0.22727 μM	SANGER
NCI-H345	Growth Inhibition Assay				IC50=0.23805 μM	SANGER
OPM-2	Growth Inhibition Assay				IC50=0.23882 μM	SANGER
LB1047-RCC	Growth Inhibition Assay				IC50=0.2441 μM	SANGER
CTB-1	Growth Inhibition Assay				IC50=0.24493 μM	SANGER
A3-KAW	Growth Inhibition Assay				IC50=0.25341 μM	SANGER
SF126	Growth Inhibition Assay				IC50=0.25383 μM	SANGER
KARPAS-422	Growth Inhibition Assay				IC50=0.25435 μM	SANGER
MEG-01	Growth Inhibition Assay				IC50=0.25673 μM	SANGER
NCI-H209	Growth Inhibition Assay				IC50=0.26374 μM	SANGER
SBC-1	Growth Inhibition Assay				IC50=0.265 μM	SANGER
K5	Growth Inhibition Assay				IC50=0.26984 μM	SANGER
QIMR-WIL	Growth Inhibition Assay				IC50=0.27155 μM	SANGER
NMC-G1	Growth Inhibition Assay				IC50=0.28217 μM	SANGER
IST-MES1	Growth Inhibition Assay				IC50=0.29238 μM	SANGER
SW684	Growth Inhibition Assay				IC50=0.30047 μM	SANGER
MV-4-11	Growth Inhibition Assay				IC50=0.30788 μM	SANGER
LAN-6	Growth Inhibition Assay				IC50=0.31572 μM	SANGER
RH-1	Growth Inhibition Assay				IC50=0.31871 μM	SANGER
CP66-MEL	Growth Inhibition Assay				IC50=0.31878 μM	SANGER
EC-GI-10	Growth Inhibition Assay				IC50=0.32987 μM	SANGER
GDM-1	Growth Inhibition Assay				IC50=0.33059 μM	SANGER
IST-SL1	Growth Inhibition Assay				IC50=0.34914 μM	SANGER
KMOE-2	Growth Inhibition Assay				IC50=0.35175 μM	SANGER
OS-RC-2	Growth Inhibition Assay				IC50=0.35544 μM	SANGER
HDLM-2	Growth Inhibition Assay				IC50=0.37814 μM	SANGER
DSH1	Growth Inhibition Assay				IC50=0.38631 μM	SANGER
LS-1034	Growth Inhibition Assay				IC50=0.38954 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay				IC50=0.39197 μM	SANGER
GOTO	Growth Inhibition Assay				IC50=0.42118 μM	SANGER
MRK-nu-1	Growth Inhibition Assay				IC50=0.42205 μM	SANGER
SK-MM-2	Growth Inhibition Assay				IC50=0.43442 μM	SANGER
BOKU	Growth Inhibition Assay				IC50=0.43792 μM	SANGER
NOMO-1	Growth Inhibition Assay				IC50=0.4386 μM	SANGER
J-RT3-T3-5	Growth Inhibition Assay				IC50=0.44878 μM	SANGER
COLO-668	Growth Inhibition Assay				IC50=0.45668 μM	SANGER
SF539	Growth Inhibition Assay				IC50=0.48684 μM	SANGER
LB2518-MEL	Growth Inhibition Assay				IC50=0.49703 μM	SANGER
TE-441-T	Growth Inhibition Assay				IC50=0.5012 μM	SANGER
MDA-MB-134-VI	Growth Inhibition Assay				IC50=0.50921 μM	SANGER
SCC-3	Growth Inhibition Assay				IC50=0.51873 μM	SANGER
KLE	Growth Inhibition Assay				IC50=0.52171 μM	SANGER
LB2241-RCC	Growth Inhibition Assay				IC50=0.52525 μM	SANGER
NCI-H1417	Growth Inhibition Assay				IC50=0.53435 μM	SANGER
NCI-H2081	Growth Inhibition Assay				IC50=0.58611 μM	SANGER
NCI-H1522	Growth Inhibition Assay				IC50=0.59383 μM	SANGER
NCI-H889	Growth Inhibition Assay				IC50=0.59844 μM	SANGER
CGTH-W-1	Growth Inhibition Assay				IC50=0.60755 μM	SANGER
EB-3	Growth Inhibition Assay				IC50=0.61153 μM	SANGER
D-336MG	Growth Inhibition Assay				IC50=0.61791 μM	SANGER
LC-1F	Growth Inhibition Assay				IC50=0.62592 μM	SANGER
MHH-NB-11	Growth Inhibition Assay				IC50=0.63801 μM	SANGER
SK-N-FI	Growth Inhibition Assay				IC50=0.6391 μM	SANGER
NCI-H69	Growth Inhibition Assay				IC50=0.64879 μM	SANGER
SCH	Growth Inhibition Assay				IC50=0.66023 μM	SANGER
LS-513	Growth Inhibition Assay				IC50=0.67259 μM	SANGER
CP67-MEL	Growth Inhibition Assay				IC50=0.67596 μM	SANGER
GCIY	Growth Inhibition Assay				IC50=0.70363 μM	SANGER
SHP-77	Growth Inhibition Assay				IC50=0.70734 μM	SANGER
EHEB	Growth Inhibition Assay				IC50=0.71854 μM	SANGER
D-247MG	Growth Inhibition Assay				IC50=0.73232 μM	SANGER
Raji	Growth Inhibition Assay				IC50=0.74989 μM	SANGER
MPP-89	Growth Inhibition Assay				IC50=0.75978 μM	SANGER
EKVX	Growth Inhibition Assay				IC50=0.79073 μM	SANGER
HCC2218	Growth Inhibition Assay				IC50=0.79131 μM	SANGER
KNS-81-FD	Growth Inhibition Assay				IC50=0.81011 μM	SANGER
HCC2157	Growth Inhibition Assay				IC50=0.84951 μM	SANGER
BT-474	Growth Inhibition Assay				IC50=0.88854 μM	SANGER
NCI-H748	Growth Inhibition Assay				IC50=0.912 μM	SANGER
EW-24	Growth Inhibition Assay				IC50=0.92002 μM	SANGER
D-263MG	Growth Inhibition Assay				IC50=0.94512 μM	SANGER
OMC-1	Growth Inhibition Assay				IC50=0.96373 μM	SANGER
NCI-H2196	Growth Inhibition Assay				IC50=0.97777 μM	SANGER
HAL-01	Growth Inhibition Assay				IC50=0.99872 μM	SANGER
NCI-H2107	Growth Inhibition Assay				IC50=1.01854 μM	SANGER
LB996-RCC	Growth Inhibition Assay				IC50=1.08051 μM	SANGER
NCI-H1395	Growth Inhibition Assay				IC50=1.1067 μM	SANGER
CHP-126	Growth Inhibition Assay				IC50=1.16199 μM	SANGER
NB69	Growth Inhibition Assay				IC50=1.26148 μM	SANGER
CAS-1	Growth Inhibition Assay				IC50=1.34231 μM	SANGER
JVM-3	Growth Inhibition Assay				IC50=1.47855 μM	SANGER
DMS-153	Growth Inhibition Assay				IC50=1.57674 μM	SANGER
SK-MEL-2	Growth Inhibition Assay				IC50=1.71789 μM	SANGER
NCI-H1155	Growth Inhibition Assay				IC50=1.73676 μM	SANGER
NCI-H1092	Growth Inhibition Assay				IC50=1.76182 μM	SANGER
LU-165	Growth Inhibition Assay				IC50=1.86476 μM	SANGER
HL-60	Growth Inhibition Assay				IC50=1.99908 μM	SANGER
REH	Growth Inhibition Assay				IC50=2.00582 μM	SANGER
JVM-2	Growth Inhibition Assay				IC50=2.06135 μM	SANGER
MN-60	Growth Inhibition Assay				IC50=2.17308 μM	SANGER
SCC-15	Growth Inhibition Assay				IC50=2.2027 μM	SANGER
SNU-C1	Growth Inhibition Assay				IC50=2.21343 μM	SANGER
SK-MEL-1	Growth Inhibition Assay				IC50=2.32047 μM	SANGER
TGW	Growth Inhibition Assay				IC50=2.35027 μM	SANGER
CA46	Growth Inhibition Assay				IC50=2.75967 μM	SANGER
NCI-H23	Growth Inhibition Assay				IC50=2.80791 μM	SANGER
MMAC-SF	Growth Inhibition Assay				IC50=2.86628 μM	SANGER
NCI-H2171	Growth Inhibition Assay				IC50=3.03448 μM	SANGER
A704	Growth Inhibition Assay				IC50=3.14194 μM	SANGER
DB	Growth Inhibition Assay				IC50=3.25576 μM	SANGER
NCI-H719	Growth Inhibition Assay				IC50=3.30384 μM	SANGER
MC-CAR	Growth Inhibition Assay				IC50=3.54817 μM	SANGER
SIMA	Growth Inhibition Assay				IC50=3.58416 μM	SANGER
SW872	Growth Inhibition Assay				IC50=3.78101 μM	SANGER
HCC1187	Growth Inhibition Assay				IC50=3.78315 μM	SANGER
EW-13	Growth Inhibition Assay				IC50=3.83417 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay				IC50=4.21999 μM	SANGER
NCI-H226	Growth Inhibition Assay				IC50=4.33606 μM	SANGER
RPMI-8866	Growth Inhibition Assay				IC50=4.36029 μM	SANGER
OCI-AML2	Growth Inhibition Assay				IC50=4.5523 μM	SANGER
LU-65	Growth Inhibition Assay				IC50=4.93033 μM	SANGER
SK-N-DZ	Growth Inhibition Assay				IC50=5.63465 μM	SANGER
NB14	Growth Inhibition Assay				IC50=5.97135 μM	SANGER
COLO-829	Growth Inhibition Assay				IC50=6.33359 μM	SANGER
MHH-CALL-2	Growth Inhibition Assay				IC50=6.51508 μM	SANGER
NCI-H1770	Growth Inhibition Assay				IC50=6.66904 μM	SANGER
ECC4	Growth Inhibition Assay				IC50=6.82179 μM	SANGER
A498	Growth Inhibition Assay				IC50=6.87192 μM	SANGER
DMS-79	Growth Inhibition Assay				IC50=7.04512 μM	SANGER
P30-OHK	Growth Inhibition Assay				IC50=7.21906 μM	SANGER
D-502MG	Growth Inhibition Assay				IC50=7.9836 μM	SANGER
RCC10RGB	Growth Inhibition Assay				IC50=8.0628 μM	SANGER
U-698-M	Growth Inhibition Assay				IC50=8.29226 μM	SANGER
BB49-HNC	Growth Inhibition Assay				IC50=9.42265 μM	SANGER
ES1	Growth Inhibition Assay				IC50=9.68956 μM	SANGER
MFM-223	Growth Inhibition Assay				IC50=10.9927 μM	SANGER
C2BBe1	Growth Inhibition Assay				IC50=11.3523 μM	SANGER
EB2	Growth Inhibition Assay				IC50=12.6881 μM	SANGER
C8166	Growth Inhibition Assay				IC50=13.8303 μM	SANGER
ES3	Growth Inhibition Assay				IC50=13.9977 μM	SANGER
NCI-H1650	Growth Inhibition Assay				IC50=16.3765 μM	SANGER
Mo-T	Growth Inhibition Assay				IC50=17.4029 μM	SANGER
NB7	Growth Inhibition Assay				IC50=17.7467 μM	SANGER
ES7	Growth Inhibition Assay				IC50=19.5507 μM	SANGER
ES5	Growth Inhibition Assay				IC50=21.7671 μM	SANGER
MSTO-211H	Growth Inhibition Assay				IC50=21.8858 μM	SANGER
U-87-MG	Growth Inhibition Assay				IC50=25.1966 μM	SANGER
THP-1	Growth Inhibition Assay				IC50=29.7201 μM	SANGER
NB10	Growth Inhibition Assay				IC50=30.2694 μM	SANGER
NH-12	Growth Inhibition Assay				IC50=33.2017 μM	SANGER
COLO-824	Growth Inhibition Assay				IC50=34.1006 μM	SANGER
SKM-1	Growth Inhibition Assay				IC50=37.8422 μM	SANGER
NCI-H1838	Growth Inhibition Assay				IC50=38.3797 μM	SANGER
RL	Growth Inhibition Assay				IC50=39.2477 μM	SANGER
COLO-800	Growth Inhibition Assay				IC50=40.0773 μM	SANGER
KG-1	Growth Inhibition Assay				IC50=40.8955 μM	SANGER
TUR	Growth Inhibition Assay				IC50=41.6399 μM	SANGER
LNCaP-Clone-FGC	Growth Inhibition Assay				IC50=41.9017 μM	SANGER
NCI-H322M	Growth Inhibition Assay				IC50=42.5984 μM	SANGER
LNCaP	Growth Inhibition Assay				IC50=91.3 nM	25505174
C4-2	Growth Inhibition Assay				IC50=8 nM	25505174
JURKAT	Growth Inhibition Assay		24 h		IC50=416.66 nM	24519995
MOLT-4	Growth Inhibition Assay		24 h		IC50=2853.5 nM	24519995
REH	Growth Inhibition Assay		24 h		IC50=287.68 nM	24519995
NALM-6	Growth Inhibition Assay		24 h		IC50=34330 nM	24519995
RS 4;11	Growth Inhibition Assay		24 h		IC50=519.05 nM	24519995
697	Growth Inhibition Assay		24 h		IC50=2107.1 nM	24519995
SIL-ALL	Growth Inhibition Assay		24 h		IC50=199.77 nM	24519995
CEM	Growth Inhibition Assay		24 h		IC50=52.18 nM	24519995
P12	Growth Inhibition Assay		24 h		IC50=39.27 nM	24519995
NALM-16	Growth Inhibition Assay		24 h		IC50=96.28 nM	24519995
JURKAT	Growth Inhibition Assay		48 h		IC50=14.84 nM	24519995
MOLT-4	Growth Inhibition Assay		48 h		IC50=26.6 nM	24519995
REH	Growth Inhibition Assay		48 h		IC50=44.71 nM	24519995
NALM-6	Growth Inhibition Assay		48 h		IC50=23.26 nM	24519995
RS 4;11	Growth Inhibition Assay		48 h		IC50=164.28 nM	24519995
697	Growth Inhibition Assay		48 h		IC50=305.3 nM	24519995
SIL-ALL	Growth Inhibition Assay		48 h		IC50=74.62 nM	24519995
CEM	Growth Inhibition Assay		48 h		IC50=24.55 nM	24519995
P12	Growth Inhibition Assay		48 h		IC50=18.46 nM	24519995
NALM-16	Growth Inhibition Assay		48 h		IC50=63.24 nM	24519995
JURKAT	Growth Inhibition Assay		72 h		IC50=3.65 nM	24519995
MOLT-4	Growth Inhibition Assay		72 h		IC50=7.39 nM	24519995
REH	Growth Inhibition Assay		72 h		IC50=16.01 nM	24519995
NALM-6	Growth Inhibition Assay		72 h		IC50=1.78 nM	24519995
RS 4;11	Growth Inhibition Assay		72 h		IC50=4.38 nM	24519995
697	Growth Inhibition Assay		72 h		IC50=74.28 nM	24519995
SIL-ALL	Growth Inhibition Assay		72 h		IC50=7.2 nM	24519995
CEM	Growth Inhibition Assay		72 h		IC50=5.42 nM	24519995
P12	Growth Inhibition Assay		72 h		IC50=6.37 nM	24519995
NALM-16	Growth Inhibition Assay		72 h		IC50=77.73 nM	24519995
Y79	Apoptosis Assay	1-50 nM	12/24 h	DMSO	induced apoptosis which can be enhanced by HT	24366665
WER-Rb-1	Apoptosis Assay	1-50 nM	12/24 h	DMSO	induced apoptosis which can be enhanced by HT	24366665
G7	Growth Inhibition Assay				IC50=3.3 nM	24204733
G166	Growth Inhibition Assay				IC50=7.0 nM	24204733
CB660	Growth Inhibition Assay				IC50=6.4 nM	24204733
CB1117	Growth Inhibition Assay				IC50=15.6 nM	24204733
KB-3-1	Growth Inhibition Assay				IC50=1.48 ± 0.53 nM	23962445
KB-8-5-11	Growth Inhibition Assay				IC50=5.01 ± 2.01 nM	23962445
KB-C-1	Growth Inhibition Assay				IC50=16.76 ± 4.51 nM	23962445
KB-V-1	Growth Inhibition Assay				IC50=281.24 ± 31.57 nM	23962445
OVCAR-8	Growth Inhibition Assay				IC50=7.19 ± 3.60 nM	23962445
NCI-ADR-RES	Growth Inhibition Assay				IC50=1273.30 ± 191.20 nM	23962445
MCF7	Growth Inhibition Assay				IC50=5.11 ± 1.47 nM	23962445
MCF7-FLV1000	Growth Inhibition Assay				IC50=393.18 ± 74.83 nM	23962445
S1	Growth Inhibition Assay				IC50=24.30 ± 4.75 nM	23962445
S1-M1-80	Growth Inhibition Assay				IC50=261.06 ± 48.25 nM	23962445
CORL-23/P	Growth Inhibition Assay				IC50=4.38 ± 1.25 nM	23962445
CORL-23/R	Growth Inhibition Assay				IC50=5.16 ± 1.83 nM	23962445
NIH3T3	Growth Inhibition Assay				IC50=40.60 ± 4.97 nM	23962445
NIH3T3-G185	Growth Inhibition Assay				IC50=2413.40 ± 423.66 nM	23962445
pcDNA-HEK293	Growth Inhibition Assay				IC50=2.75 ± 0.67 nM	23962445
MDR19-HEK293	Growth Inhibition Assay				IC50=85.50 ± 13.67 nM	23962445
R482-HEK293	Growth Inhibition Assay				IC50=25.97 ± 4.95 nM	23962445
MRP1-HEK293	Growth Inhibition Assay				IC50=2.99 ± 1.49 nM	23962445
SF188	Growth Inhibition Assay	10-100 nM	24-96 h	DMSO	inhibits cell growth in both time- and concentration- depedent manner	23887645
T98G	Growth Inhibition Assay	10-100 nM	24-96 h	DMSO	inhibits cell growth in concentration- depedent manner	23887645
DU145	Growth Inhibition Assay			DMSO	IC50∼60 nM	23884428
LNCaP	Growth Inhibition Assay			DMSO	IC50∼75 nM	23884428
PC3	Growth Inhibition Assay			DMSO	IC50∼175 nM	23884428
RT4	Growth Inhibition Assay				IC50=27.21 nM	23792639
5637	Growth Inhibition Assay				IC50=45.47 nM	23792639
T24	Growth Inhibition Assay				IC50=79.12 nM	23792639
MCF7	Function Assay	100 nM	1 h	DMSO	reduces the induction of Greb1, Sgk1, Ps2, Serpina3, and Wisp2	23770244
KB-V1	Growth Inhibition Assay				IC50=3.92 μM	23593196
Hec50co	Growth Inhibition Assay				IC50=5 nM	23146687
MDA-MB-468	Apoptosis Assay	1/5/10 nM	24/48/72 h	DMSO	induces apoptosis in a dose-dependent manner	23144294
MCF10A	Apoptosis Assay	1/5/10 nM	24/48/72 h	DMSO	induces apoptosis in a dose-dependent manner	23144294
Huh-7	Growth Inhibition Assay	1/10/100/1000 nM	48 h		decreases the cell viability dose-dependently	22745587
Daoy	Growth Inhibition Assay	1.875-240 nM	72 h	DMSO	IC50=5 nM	22390279
ONS-76	Growth Inhibition Assay	1.875-240 nM	72 h	DMSO	IC50=7.5 nM	22390279
SUM 149	Growth Inhibition Assay	0-100 nM	72 h		inhibits the cell viability in a dose-dependent mannar	22309939
MDA-MB-231	Growth Inhibition Assay	0-100 nM	72 h		inhibits the cell viability in a dose-dependent mannar	22309939
HR5	Growth Inhibition Assay	0-100 nM	72 h		inhibits the cell viability in a dose-dependent mannar	22309939
BT-474-M1	Growth Inhibition Assay	0-100 nM	72 h		inhibits the cell viability in a dose-dependent mannar	22309939
AU565	Growth Inhibition Assay	0-100 nM	72 h		inhibits the cell viability in a dose-dependent mannar	22309939
T47D	Growth Inhibition Assay	0-100 nM	72 h		inhibits the cell viability in a dose-dependent mannar	22309939
MCF7	Growth Inhibition Assay	0-100 nM	72 h		inhibits the cell viability in a dose-dependent mannar	22309939
HCT116p53(+/+)	Growth Inhibition Assay	10-1000 nM	24/48 h		inhibits cell proliferation completely at 25 nM	22262171
HCT116p53(-/-)	Growth Inhibition Assay	10-1000 nM	24/48 h		inhibits cell proliferation completely at 25 nM	22262171
HeLa	Growth Inhibition Assay	10-100 nM	48 h	DMSO	IC50=52.9 nM	22080235
HeLa	Growth Inhibition Assay	10-100 nM	72 h	DMSO	IC50=50.5 nM	22080235
GBC	Growth Inhibition Assay		72 h		IC50=14.78 nM	21965739
GB-CL-1	Growth Inhibition Assay		72 h		IC50=5.22 nM	21965739
Mz-ChA-2	Growth Inhibition Assay		72 h		IC50=3.31 nM	21965739
TGBC1-TKB	Growth Inhibition Assay		144 h		IC50=6.72 nM	21965739
Wittier	Growth Inhibition Assay		72 h		IC50=3.26 nM	21965739
H-1	Growth Inhibition Assay		72 h		IC50=9.54 nM	21965739
HuH-28	Growth Inhibition Assay		72 h		IC50=11.19 nM	21965739
NEC	Growth Inhibition Assay		72 h		IC50=9.98 nM	21965739
REB	Growth Inhibition Assay		72 h		IC50=13.51 nM	21965739
CC-LP-1	Growth Inhibition Assay		72 h		IC50=5.84 nM	21965739
CC-SW-1	Growth Inhibition Assay		72 h		IC50=9.55 nM	21965739
EGI-1	Growth Inhibition Assay		72 h		IC50=10.72 nM	21965739
Sk-ChA-1	Growth Inhibition Assay		72 h		IC50=17.2 nM	21965739
TFK-1	Growth Inhibition Assay		72 h		IC50=13.45 nM	21965739
786-O	Growth Inhibition Assay	5-80 nM	96 h	HCl	suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM	21642374
A498	Growth Inhibition Assay	5-80 nM	96 h	HCl	suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM	21642374
ACHN	Growth Inhibition Assay	5-80 nM	96 h	HCl	suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM	21642374
Caki-1	Growth Inhibition Assay	5-80 nM	96 h	HCl	suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM	21642374
SN12C	Growth Inhibition Assay	5-80 nM	96 h	HCl	suppresses the proliferation in a dose-dependent manner with IC50 values of 2 to 20 nM	21642374
HMC-1.1	Growth Inhibition Assay	1-1000 nM	72 h		inhibits the cell proliferation in a dose-dependent manne	21242189
HMC-1.2	Growth Inhibition Assay	1-1000 nM	72 h		inhibits the cell proliferation in a dose-dependent manne	21242189
C2	Growth Inhibition Assay	1-1000 nM	72 h		inhibits the cell proliferation in a dose-dependent manne	21242189
CHP-212	Growth Inhibition Assay	1-125 nM	24-120 h		inhibits the cell proliferation in both time- and dose-dependent manne	21169242
IMR-32	Growth Inhibition Assay	1-125 nM	24-120 h		inhibits the cell proliferation in both time- and dose-dependent manne	21169242
Kelly	Growth Inhibition Assay	1-125 nM	24-120 h		inhibits the cell proliferation in both time- and dose-dependent manne	21169242
SH-EP	Growth Inhibition Assay	1-125 nM	24-120 h		inhibits the cell proliferation in both time- and dose-dependent manne	21169242
SH-SY5Y	Growth Inhibition Assay	1-125 nM	24-120 h		inhibits the cell proliferation in both time- and dose-dependent manne	21169242
SK-N-AS	Growth Inhibition Assay	1-125 nM	24-120 h		inhibits the cell proliferation in both time- and dose-dependent manne	21169242
SK-N-BE	Growth Inhibition Assay	1-125 nM	24-120 h		inhibits the cell proliferation in both time- and dose-dependent manne	21169242
KG1	Growth Inhibition Assay	1/10/100 nM	72 h	DMSO	inhibits the cell proliferation in both time- and dose-dependent manne	19458358
U937	Growth Inhibition Assay	1/10/100 nM	72 h	DMSO	inhibits the cell proliferation in both time- and dose-dependent manne	19458358
CAL62	Growth Inhibition Assay	0.1-100 nM	72 h	DMSO	EC50=1.4 nM	19223553
OCUT-1	Growth Inhibition Assay	0.1-100 nM	72 h	DMSO	EC50=2.3 nM	19223553
8505C	Growth Inhibition Assay	0.1-100 nM	72 h	DMSO	EC50=3.2 nM	19223553
ACT-1	Growth Inhibition Assay	0.1-100 nM	72 h	DMSO	EC50=5.4 nM	19223553
SW1736	Growth Inhibition Assay	0.1-100 nM	72 h	DMSO	EC50=5.6 nM	19223553
HEK293	Function assay		1 hr		Binding affinity to PLK1 (unknown origin) expressed in HEK293 cells after 1 hr by proprietary competition assay, Ki = 0.00022 μM.	26191363
HEK293T	Antiproliferative assay		72 hrs		Antiproliferative activity against HEK293T cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM.	28792760
MDA-MB-231	Antiproliferative assay		72 hrs		Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM.	28792760
MM1S	Antiproliferative assay		72 hrs		Antiproliferative activity against human MM1S cells measured after 72 hrs by CellTiter-Blue assay, IC50 = 0.001 μM.	28792760
TY82	Antiproliferative assay		72 hrs		Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay, IC50 = 0.001 μM.	28586718
NMC-797	Cytotoxicity assay		3 days		Cytotoxicity against BRD4 dependent human NMC-797 cells assessed as cell viability after 3 days by ATPlite assay, IC50 = 0.0107 μM.	26985285
MV4-11	Cytotoxicity assay		24 hrs		Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay, GI50 = 0.0152 μM.	26191363
BL21(DE3)	Function assay		60 mins		Inhibition of recombinant human N-terminal His6-tagged BRD4 expressed in Escherichia coli BL21(DE3) cells using biotinylated histone H4 peptide as substrate after 60 mins by AlphaScreen assay, IC50 = 0.025 μM.	28195723
BL21(DE3)	Function assay				Inhibition of human N-terminal His6-tagged BRD4-BD1 (44 to 168 residues) expressed in Escherichia coli BL21 (DE3) cells using protein thermal shift dye as fluorescence probe by differential scanning fluorimetry, IC50 = 0.025 μM.	28586718
HuH7	Antiproliferative assay		72 hrs		Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay, GI50 = 0.028 μM.	29220793
HeLa	Antiproliferative assay		72 hrs		Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay, GI50 = 0.034 μM.	29220793
HL60	Cytotoxicity assay		3 days		Cytotoxicity against BRD4 dependent human HL60 cells assessed as cell viability after 3 days by ATPlite assay, IC50 = 0.0365 μM.	26985285
A549	Antiproliferative assay		72 hrs		Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay, GI50 = 0.057 μM.	29220793
MCF7	Antiproliferative assay		72 hrs		Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay, GI50 = 0.067 μM.	29220793
K562	Antiproliferative assay		72 hrs		Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, GI50 = 0.068 μM.	29220793
MDA-MB-23	Function assay		6 hrs		Inhibition of PLK1 in human MDA-MB-23 cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot method, IC50 = 0.1 μM.	28792760
HEK293T	Function assay		6 hrs		Inhibition of PLK1 in HEK293T cells assessed as decrease in TCTP phosphorylation after 6 hrs by Western blot method, IC50 = 0.1 μM.	28792760
NCI-H1975	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H1975 cells after 72 hrs by CCK8 assay, GI50 = 0.23 μM.	29220793
BL21(DE3)	Function assay		4 hrs		Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay, IC50 = 0.25 μM.	28586718
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
Fibroblast cells	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63(6-TG R)	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Fibroblast cells	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells	29435139
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
RD	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
DU145	Apoptosis assay	100 nM	24 hrs		Induction of apoptosis in human DU145 cells assessed as increase in PARP cleavage at 100 nM after 24 hrs by immunoblotting method	25685941
HeLa	Function assay	100 nM			Inhibition of PLK1 Thr210 phosphorylation in human HeLa cells at 100 nM by immunoblotting method	25685941
DU145	Function assay	100 nM			Inhibition of PLK1 protein accumulation in human DU145 cells at 100 nM by immunoblotting method	25685941
HeLa	Function assay	100 nM			Inhibition of PLK1 protein accumulation in human HeLa cells at 100 nM by immunoblotting method	25685941
HeLa	Function assay	100 nM	18 hrs		Induction of monopolar mitotic spindles in human HeLa cells at 100 nM incubated for 18 hrs by indirect immunofluorescence microscopy	25685941
HeLa	Apoptosis assay	100 nM	24 hrs		Induction of apoptosis in human HeLa cells assessed as increase in PARP cleavage at 100 nM after 24 hrs by immunoblotting method	25685941
PC3	Function assay	100 nM	18 hrs		Induction of monopolar mitotic spindles in human PC3 cells at 100 nM incubated for 18 hrs by indirect immunofluorescence microscopy	25685941
DU145	Function assay	100 nM			Inhibition of PLK1 Thr210 phosphorylation in human DU145 cells at 100 nM by immunoblotting method	25685941
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Informations chimiques, stockage et stabilité

Poids moléculaire	521.66	Formule	C₂₈H₃₉N₇O₃	Stockage (À partir de la date de réception)	3 ans-20°Cpoudre
N° CAS	755038-02-9	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	CCC1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C

Solubilité

In vitro
Lot:

Ethanol : 104 mg/mL

DMSO : 96 mg/mL (184.02 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	4.000mg/ml (7.67mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	1.000mg/ml (1.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 5%Tween80 2 90%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	3.300mg/ml (6.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 66 mg/ml clarified DMSO stock solution to 50 μL of Tween80, mix evenly to clarify; then continue to add 900 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe de vente pour des tests personnalisés.	2.000mg/ml (3.83mM)	Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Entrez les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Entrez la formulation in vivo (Ceci nest que le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuiteμL PEG300, mélanger et clarifier, ajouter ensuiteμL Tween 80, mélanger et clarifier, ajouter ensuite μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, ajouter ensuite μL Huile de maïs, mélanger et clarifier.

Remarque : 1. Assurez-vous que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue lors de lajout précédent est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Fonctionnalités	The first potent and selective Plk1 inhibitor that induces all hallmarks of Plk1 inhibition.
Targets/IC₅₀/Ki	c-Myc PLK1 (Cell-free assay) 0.83 nM PLK2 (Cell-free assay) 3.5 nM PLK3 (Cell-free assay) 9.0 nM BRD4 (Cell-free assay) 37 nM(Kd)
In vitro	BI 2536 bloque les activités de Plk2 et Plk3 dans une moindre mesure avec des IC50 de 3,5 nM et 9,0 nM, respectivement. Dans les cellules HeLa, ce traitement composé allant de 10 à 100 nM entraîne le blocage du recrutement de la γ-tubuline et la phosphorylation d'Apc6 aux centrosomes mitotiques, l'inhibition de la libération de la cohésine des bras chromosomiques, l'induction de fuseaux monopolaires, ainsi qu'une gamme d'autres processus mitotiques dont on sait qu'ils dépendent de Plk1. Ce traitement chimique conduit à l'arrêt des cellules HeLa en G2/M, puis à un pic d'ADN sub-G1 indiquant une dégradation de l'ADN et une Apoptosis, et à l'accumulation de fragments de PARP p85 clivés de manière concentration-dépendante. Il inhibe la croissance d'un panel de 32 lignées de cellules cancéreuses humaines avec des EC50 de 2-25 nM, tout en bloquant la prolifération des cellules hTERT-RPE1 en croissance exponentielle, des cellules endothéliales de la veine ombilicale humaine (HUVECs) et des cellules rénales de rat normales (NRK) avec des EC50 de 12-31 nM. L'inhibition de Plk1 par ce composé réduit la croissance et la viabilité des cellules de carcinome thyroïdien anaplasique (ATC) telles que CAL62, OCUT-1, SW1736, 8505C et ACT-1 avec des valeurs d'EC50 de 1,4-5,6 nM.
Kinase Assay	Essai kinase in vitro de Plk1
Kinase Assay	La Plk1 humaine recombinante (résidus 1-603) est exprimée sous forme de protéine de fusion N-terminale, étiquetée GST, avec un système d'expression baculoviral et purifiée par chromatographie d'affinité avec de l'agarose-glutathion. Les tests d'activité enzymatique pour Plk1 sont effectués en présence de BI 2536 dilué en série avec 20 ng de kinase recombinante et 10 μg de caséine de lait bovin comme substrat. Les réactions de kinase sont effectuées dans un volume final de 60 μL pendant 45 minutes à 30 °C (15 mM MgCl₂, 25 mM MOPS [pH 7.0], 1 mM DTT, 1% DMSO, 7.5 mM ATP, 0.3 μCi γ-³³P-ATP). Les réactions sont terminées par l'ajout de 125 μL de TCA à 5% glacé. Après transfert des précipités sur des plaques filtrantes en cellulose à ester mixte Multi-Screen, les plaques sont lavées avec 1% de TCA et quantifiées radiométriquement. La courbe dose-réponse est utilisée pour calculer la valeur IC50.
In vivo	Administré par voie intraveineuse une ou deux fois par semaine, BI 2536 est très efficace dans divers modèles de xénogreffes avec une tolérance acceptable en inhibant la prolifération cellulaire par un arrêt mitotique, et par la suite en induisant la mort des cellules tumorales. L'administration de ce composé à 50 mg/kg une ou deux fois par semaine inhibe significativement la croissance des xénogreffes HCT 116 avec un T/C de 15% et 0,3% respectivement. Ce traitement chimique deux fois par semaine entraîne également une excellente croissance tumorale dans les modèles BxPC-3 et A549 avec un T/C de 5% et 14% respectivement.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/17291758/ [2] https://pubmed.ncbi.nlm.nih.gov/19223553/ [3] https://pubmed.ncbi.nlm.nih.gov/26191363/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	pro-caspase-8 / cleaved caspase-8 / cleaved caspase-3 / cleaved caspase-9 p-HH3 / PARP / Myc / p-Myc pMEK / MEK / pERK / ERK / pRSK1 / RSK1 pPlk1 / Plk1 / pMyt1 Aurora B / pAurora B / pAurora C / pH3 / Cyclin B1 / Securin / pBcl-XL / MPM2	27699933
Immunofluorescence	p-H2AX / propidium iodide Pericentrin / α-tubulin	22309939
Growth inhibition assay	Cell viability	21772266

Informations sur lessai clinique

(données de https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Sponsor/Collaborateurs	Date de début	Phases
NCT02215044	Terminated	Pancreatic Neoplasms	Boehringer Ingelheim	June 2007	Phase 1
NCT02211833	Completed	Carcinoma Non-Small-Cell Lung	Boehringer Ingelheim	October 2006	Phase 1
NCT00701766	Completed	Leukemia Myeloid Acute	Boehringer Ingelheim	October 2006	Phase 2
NCT00706498	Completed	Prostatic Neoplasms	Boehringer Ingelheim	September 2006	Phase 2
NCT00376623	Completed	Carcinoma Non-Small-Cell Lung	Boehringer Ingelheim	July 25 2006	Phase 2
NCT02211872	Completed	Neoplasms	Boehringer Ingelheim	August 2004	Phase 1

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

Questions fréquemment posées

Question 1:
We need to use it in preclinical studies using mice; how to formulate this compound for the in vivo study?

Réponse :
For in vivo study, DMSO should not be more than 5% because of the toxicity. It can be formulated in hydrochloric acid (0.1 N), and diluted with 0.9% NaCl for animal study according to the reference: (Supplemental Data) http://linkinghub.elsevier.com/retrieve/pii/S0960-9822(06)02671-6

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