solo para uso en investigación

CI-1040 (PD184352) MEK Inhibidor

Name: CI-1040 (PD184352)
Brand: Selleck Chemicals
SKU: S1020
Rating: 5 (142 reviews)

Cat. No.S1020

PD184352 (CI-1040) es un inhibidor no competitivo de ATP de MEK1/2 con una IC50 de 17 nM en ensayos basados en células, 100 veces más selectivo para MEK1/2 que para MEK5. PD184352 (CI-1040) induce selectivamente la apoptosis.

CI-1040 (PD184352) MEK Inhibidor Chemical Structure

Estructura química

Peso molecular: 478.67

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.96%

99.96

Dianas relacionadas	ERK p38 MAPK Raf JNK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Otros MEK Inhibidores	PD0325901 (Mirdametinib) U0126-EtOH PD 98059 (E/Z)-BIX02189 Pimasertib (AS-703026) Refametinib (RDEA119) TAK-733 AZD8330 GDC-0623 SL-327

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
PC-3	Growth Inhibition Assay			IC50=24.0526 μM	SANGER
VM-CUB-1	Growth Inhibition Assay			IC50=23.7341 μM	SANGER
LC-2-ad	Growth Inhibition Assay			IC50=23.6147 μM	SANGER
A704	Growth Inhibition Assay			IC50=23.6103 μM	SANGER
DMS-114	Growth Inhibition Assay			IC50=23.5765 μM	SANGER
EKVX	Growth Inhibition Assay			IC50=23.3909 μM	SANGER
SNU-449	Growth Inhibition Assay			IC50=23.329 μM	SANGER
HCC1806	Growth Inhibition Assay			IC50=23.0583 μM	SANGER
CaR-1	Growth Inhibition Assay			IC50=23.0213 μM	SANGER
NCI-H441	Growth Inhibition Assay			IC50=22.5689 μM	SANGER
TI-73	Growth Inhibition Assay			IC50=22.328 μM	SANGER
NCI-H1755	Growth Inhibition Assay			IC50=21.6741 μM	SANGER
A498	Growth Inhibition Assay			IC50=21.5312 μM	SANGER
CFPAC-1	Growth Inhibition Assay			IC50=21.3858 μM	SANGER
ChaGo-K-1	Growth Inhibition Assay			IC50=21.3627 μM	SANGER
KP-4	Growth Inhibition Assay			IC50=21.1196 μM	SANGER
Becker	Growth Inhibition Assay			IC50=21.1118 μM	SANGER
UMC-11	Growth Inhibition Assay			IC50=20.9164 μM	SANGER
TE-6	Growth Inhibition Assay			IC50=20.8067 μM	SANGER
SF539	Growth Inhibition Assay			IC50=20.5172 μM	SANGER
FTC-133	Growth Inhibition Assay			IC50=20.4703 μM	SANGER
NCI-H226	Growth Inhibition Assay			IC50=20.4399 μM	SANGER
NCI-H1048	Growth Inhibition Assay			IC50=20.3266 μM	SANGER
Calu-3	Growth Inhibition Assay			IC50=19.4237 μM	SANGER
SF126	Growth Inhibition Assay			IC50=19.3502 μM	SANGER
NTERA-S-cl-D1	Growth Inhibition Assay			IC50=19.2007 μM	SANGER
SW1573	Growth Inhibition Assay			IC50=19.1969 μM	SANGER
SNU-387	Growth Inhibition Assay			IC50=19.1889 μM	SANGER
ETK-1	Growth Inhibition Assay			IC50=19.1827 μM	SANGER
HuO9	Growth Inhibition Assay			IC50=19.1379 μM	SANGER
RO82-W-1	Growth Inhibition Assay			IC50=18.8288 μM	SANGER
D-502MG	Growth Inhibition Assay			IC50=18.8139 μM	SANGER
LS-123	Growth Inhibition Assay			IC50=18.7901 μM	SANGER
OC-314	Growth Inhibition Assay			IC50=18.7384 μM	SANGER
Ramos-2G6-4C10	Growth Inhibition Assay			IC50=18.5927 μM	SANGER
SW962	Growth Inhibition Assay			IC50=18.5702 μM	SANGER
SW982	Growth Inhibition Assay			IC50=18.5649 μM	SANGER
KYSE-410	Growth Inhibition Assay			IC50=18.4577 μM	SANGER
HT-3	Growth Inhibition Assay			IC50=18.3977 μM	SANGER
CAL-85-1	Growth Inhibition Assay			IC50=18.1809 μM	SANGER
BB30-HNC	Growth Inhibition Assay			IC50=18.0318 μM	SANGER
D-247MG	Growth Inhibition Assay			IC50=17.9247 μM	SANGER
SCC-15	Growth Inhibition Assay			IC50=17.8473 μM	SANGER
BB49-HNC	Growth Inhibition Assay			IC50=17.5686 μM	SANGER
KYSE-70	Growth Inhibition Assay			IC50=17.289 μM	SANGER
NKM-1	Growth Inhibition Assay			IC50=17.0189 μM	SANGER
NCI-H23	Growth Inhibition Assay			IC50=16.6078 μM	SANGER
NCI-H2228	Growth Inhibition Assay			IC50=16.5158 μM	SANGER
BxPC-3	Growth Inhibition Assay			IC50=16.2856 μM	SANGER
VMRC-RCZ	Growth Inhibition Assay			IC50=16.2592 μM	SANGER
NCI-H1299	Growth Inhibition Assay			IC50=16.2291 μM	SANGER
A204	Growth Inhibition Assay			IC50=16.2006 μM	SANGER
NCI-H28	Growth Inhibition Assay			IC50=16.0856 μM	SANGER
G-401	Growth Inhibition Assay			IC50=15.9649 μM	SANGER
HOP-62	Growth Inhibition Assay			IC50=15.9597 μM	SANGER
TGBC11TKB	Growth Inhibition Assay			IC50=15.9414 μM	SANGER
SAS	Growth Inhibition Assay			IC50=15.9373 μM	SANGER
LU-134-A	Growth Inhibition Assay			IC50=15.9018 μM	SANGER
OCI-AML2	Growth Inhibition Assay			IC50=15.7614 μM	SANGER
ES3	Growth Inhibition Assay			IC50=15.536 μM	SANGER
PC-14	Growth Inhibition Assay			IC50=15.4866 μM	SANGER
Detroit562	Growth Inhibition Assay			IC50=15.4547 μM	SANGER
SCC-4	Growth Inhibition Assay			IC50=15.4103 μM	SANGER
NCI-H1563	Growth Inhibition Assay			IC50=15.349 μM	SANGER
AM-38	Growth Inhibition Assay			IC50=15.2717 μM	SANGER
EC-GI-10	Growth Inhibition Assay			IC50=15.2357 μM	SANGER
OE33	Growth Inhibition Assay			IC50=15.1711 μM	SANGER
OVCAR-4	Growth Inhibition Assay			IC50=15.1424 μM	SANGER
U-87-MG	Growth Inhibition Assay			IC50=15.0897 μM	SANGER
MKN7	Growth Inhibition Assay			IC50=15.0093 μM	SANGER
NCI-H661	Growth Inhibition Assay			IC50=14.959 μM	SANGER
LB831-BLC	Growth Inhibition Assay			IC50=14.8934 μM	SANGER
BT-549	Growth Inhibition Assay			IC50=14.8284 μM	SANGER
NCI-H2347	Growth Inhibition Assay			IC50=14.823 μM	SANGER
OVCAR-8	Growth Inhibition Assay			IC50=14.7201 μM	SANGER
NCI-H630	Growth Inhibition Assay			IC50=14.6568 μM	SANGER
U-118-MG	Growth Inhibition Assay			IC50=14.631 μM	SANGER
LS-1034	Growth Inhibition Assay			IC50=14.6152 μM	SANGER
BALL-1	Growth Inhibition Assay			IC50=14.4665 μM	SANGER
Capan-2	Growth Inhibition Assay			IC50=14.3714 μM	SANGER
QIMR-WIL	Growth Inhibition Assay			IC50=14.3412 μM	SANGER
HC-1	Growth Inhibition Assay			IC50=14.2087 μM	SANGER
NCI-H2030	Growth Inhibition Assay			IC50=14.1465 μM	SANGER
NB17	Growth Inhibition Assay			IC50=14.085 μM	SANGER
GCT	Growth Inhibition Assay			IC50=13.9697 μM	SANGER
OS-RC-2	Growth Inhibition Assay			IC50=13.9501 μM	SANGER
GCIY	Growth Inhibition Assay			IC50=13.6927 μM	SANGER
SF268	Growth Inhibition Assay			IC50=13.6326 μM	SANGER
NCI-H2009	Growth Inhibition Assay			IC50=13.5919 μM	SANGER
CAPAN-1	Growth Inhibition Assay			IC50=13.5514 μM	SANGER
NCI-H2452	Growth Inhibition Assay			IC50=13.2175 μM	SANGER
OAW-42	Growth Inhibition Assay			IC50=13.1937 μM	SANGER
NCI-H1092	Growth Inhibition Assay			IC50=13.162 μM	SANGER
SW13	Growth Inhibition Assay			IC50=13.1165 μM	SANGER
8-MG-BA	Growth Inhibition Assay			IC50=13.0455 μM	SANGER
ATN-1	Growth Inhibition Assay			IC50=13.0184 μM	SANGER
OVCAR-3	Growth Inhibition Assay			IC50=12.9567 μM	SANGER
LXF-289	Growth Inhibition Assay			IC50=12.9531 μM	SANGER
HT	Growth Inhibition Assay			IC50=12.8346 μM	SANGER
769-P	Growth Inhibition Assay			IC50=12.7924 μM	SANGER
BEN	Growth Inhibition Assay			IC50=12.6143 μM	SANGER
HSC-2	Growth Inhibition Assay			IC50=12.5996 μM	SANGER
TCCSUP	Growth Inhibition Assay			IC50=12.5757 μM	SANGER
BHY	Growth Inhibition Assay			IC50=12.5307 μM	SANGER
KYSE-510	Growth Inhibition Assay			IC50=12.5079 μM	SANGER
ES7	Growth Inhibition Assay			IC50=12.2724 μM	SANGER
NCI-H1703	Growth Inhibition Assay			IC50=12.2616 μM	SANGER
GI-ME-N	Growth Inhibition Assay			IC50=12.2163 μM	SANGER
NOS-1	Growth Inhibition Assay			IC50=12.1352 μM	SANGER
SW1990	Growth Inhibition Assay			IC50=12.0911 μM	SANGER
SJSA-1	Growth Inhibition Assay			IC50=12.0735 μM	SANGER
HLE	Growth Inhibition Assay			IC50=12.0585 μM	SANGER
LB373-MEL-D	Growth Inhibition Assay			IC50=12.0533 μM	SANGER
KALS-1	Growth Inhibition Assay			IC50=12.0016 μM	SANGER
D-336MG	Growth Inhibition Assay			IC50=11.9075 μM	SANGER
KYSE-270	Growth Inhibition Assay			IC50=11.8745 μM	SANGER
KOSC-2	Growth Inhibition Assay			IC50=11.6222 μM	SANGER
S-117	Growth Inhibition Assay			IC50=11.4896 μM	SANGER
KYSE-180	Growth Inhibition Assay			IC50=11.482 μM	SANGER
KYSE-450	Growth Inhibition Assay			IC50=11.4057 μM	SANGER
SW837	Growth Inhibition Assay			IC50=11.3506 μM	SANGER
YH-13	Growth Inhibition Assay			IC50=11.3267 μM	SANGER
SF295	Growth Inhibition Assay			IC50=11.3104 μM	SANGER
KS-1	Growth Inhibition Assay			IC50=11.2619 μM	SANGER
SW756	Growth Inhibition Assay			IC50=11.2154 μM	SANGER
SBC-5	Growth Inhibition Assay			IC50=11.1467 μM	SANGER
U251	Growth Inhibition Assay			IC50=11.042 μM	SANGER
DJM-1	Growth Inhibition Assay			IC50=11.0379 μM	SANGER
MOLT-16	Growth Inhibition Assay			IC50=10.8113 μM	SANGER
NEC8	Growth Inhibition Assay			IC50=10.7773 μM	SANGER
NCI-H1623	Growth Inhibition Assay			IC50=10.6379 μM	SANGER
GMS-10	Growth Inhibition Assay			IC50=10.6094 μM	SANGER
CCRF-CEM	Growth Inhibition Assay			IC50=10.5684 μM	SANGER
VA-ES-BJ	Growth Inhibition Assay			IC50=10.567 μM	SANGER
KE-37	Growth Inhibition Assay			IC50=10.5272 μM	SANGER
KYSE-520	Growth Inhibition Assay			IC50=10.52 μM	SANGER
MKN28	Growth Inhibition Assay			IC50=10.518 μM	SANGER
SK-NEP-1	Growth Inhibition Assay			IC50=10.4981 μM	SANGER
MDA-MB-175-VII	Growth Inhibition Assay			IC50=10.48 μM	SANGER
KARPAS-45	Growth Inhibition Assay			IC50=10.2795 μM	SANGER
NCI-H720	Growth Inhibition Assay			IC50=10.1989 μM	SANGER
NCI-H1573	Growth Inhibition Assay			IC50=10.1574 μM	SANGER
MSTO-211H	Growth Inhibition Assay			IC50=9.95529 μM	SANGER
KGN	Growth Inhibition Assay			IC50=9.83795 μM	SANGER
YKG-1	Growth Inhibition Assay			IC50=9.75033 μM	SANGER
P30-OHK	Growth Inhibition Assay			IC50=9.65316 μM	SANGER
639-V	Growth Inhibition Assay			IC50=9.64388 μM	SANGER
SW1417	Growth Inhibition Assay			IC50=9.56837 μM	SANGER
NCI-H1792	Growth Inhibition Assay			IC50=9.45219 μM	SANGER
MKN45	Growth Inhibition Assay			IC50=9.45065 μM	SANGER
HCC1937	Growth Inhibition Assay			IC50=9.29091 μM	SANGER
MEG-01	Growth Inhibition Assay			IC50=9.24931 μM	SANGER
DK-MG	Growth Inhibition Assay			IC50=9.21191 μM	SANGER
TE-12	Growth Inhibition Assay			IC50=9.03367 μM	SANGER
NCI-H2126	Growth Inhibition Assay			IC50=9.00826 μM	SANGER
T98G	Growth Inhibition Assay			IC50=8.99846 μM	SANGER
SK-UT-1	Growth Inhibition Assay			IC50=8.97683 μM	SANGER
SW954	Growth Inhibition Assay			IC50=8.96978 μM	SANGER
NCI-H1693	Growth Inhibition Assay			IC50=8.9217 μM	SANGER
RKO	Growth Inhibition Assay			IC50=8.89057 μM	SANGER
MS-1	Growth Inhibition Assay			IC50=8.87517 μM	SANGER
ES4	Growth Inhibition Assay			IC50=8.86884 μM	SANGER
SBC-1	Growth Inhibition Assay			IC50=8.86645 μM	SANGER
K-562	Growth Inhibition Assay			IC50=8.83957 μM	SANGER
SK-N-FI	Growth Inhibition Assay			IC50=8.81379 μM	SANGER
DBTRG-05MG	Growth Inhibition Assay			IC50=8.74859 μM	SANGER
CAL-12T	Growth Inhibition Assay			IC50=8.65753 μM	SANGER
A673	Growth Inhibition Assay			IC50=8.63202 μM	SANGER
CAKI-1	Growth Inhibition Assay			IC50=8.57222 μM	SANGER
TE-5	Growth Inhibition Assay			IC50=8.42429 μM	SANGER
NCI-H1581	Growth Inhibition Assay			IC50=8.26323 μM	SANGER
DOHH-2	Growth Inhibition Assay			IC50=8.20095 μM	SANGER
EW-16	Growth Inhibition Assay			IC50=8.08445 μM	SANGER
ECC10	Growth Inhibition Assay			IC50=8.03395 μM	SANGER
IST-MEL1	Growth Inhibition Assay			IC50=8.00406 μM	SANGER
TGBC1TKB	Growth Inhibition Assay			IC50=7.89398 μM	SANGER
COLO-678	Growth Inhibition Assay			IC50=7.71076 μM	SANGER
SCC-25	Growth Inhibition Assay			IC50=7.709 μM	SANGER
NB14	Growth Inhibition Assay			IC50=7.66642 μM	SANGER
NCI-H1355	Growth Inhibition Assay			IC50=7.58635 μM	SANGER
U-266	Growth Inhibition Assay			IC50=7.56286 μM	SANGER
LU-135	Growth Inhibition Assay			IC50=7.55939 μM	SANGER
GR-ST	Growth Inhibition Assay			IC50=7.40174 μM	SANGER
BE-13	Growth Inhibition Assay			IC50=7.33834 μM	SANGER
SK-MEL-30	Growth Inhibition Assay			IC50=7.25083 μM	SANGER
COR-L23	Growth Inhibition Assay			IC50=7.2442 μM	SANGER
DoTc2-4510	Growth Inhibition Assay			IC50=7.1215 μM	SANGER
8305C	Growth Inhibition Assay			IC50=7.09995 μM	SANGER
ACHN	Growth Inhibition Assay			IC50=7.02943 μM	SANGER
HuCCT1	Growth Inhibition Assay			IC50=7.01037 μM	SANGER
SW48	Growth Inhibition Assay			IC50=6.9451 μM	SANGER
SW1088	Growth Inhibition Assay			IC50=6.91913 μM	SANGER
MFE-280	Growth Inhibition Assay			IC50=6.85983 μM	SANGER
MHH-NB-11	Growth Inhibition Assay			IC50=6.85002 μM	SANGER
HCT-116	Growth Inhibition Assay			IC50=6.81264 μM	SANGER
Calu-6	Growth Inhibition Assay			IC50=6.79698 μM	SANGER
AN3-CA	Growth Inhibition Assay			IC50=6.68641 μM	SANGER
COR-L105	Growth Inhibition Assay			IC50=6.65275 μM	SANGER
NCI-H2122	Growth Inhibition Assay			IC50=6.61528 μM	SANGER
D-566MG	Growth Inhibition Assay			IC50=6.54303 μM	SANGER
A172	Growth Inhibition Assay			IC50=6.49176 μM	SANGER
NCI-H1975	Growth Inhibition Assay			IC50=6.47215 μM	SANGER
TK10	Growth Inhibition Assay			IC50=6.32604 μM	SANGER
PANC-10-05	Growth Inhibition Assay			IC50=6.28363 μM	SANGER
A431	Growth Inhibition Assay			IC50=6.24296 μM	SANGER
MV-4-11	Growth Inhibition Assay			IC50=6.23199 μM	SANGER
RPMI-8866	Growth Inhibition Assay			IC50=6.21313 μM	SANGER
NCI-H1304	Growth Inhibition Assay			IC50=6.1994 μM	SANGER
NCI-H1666	Growth Inhibition Assay			IC50=6.08461 μM	SANGER
KYSE-140	Growth Inhibition Assay			IC50=6.02182 μM	SANGER
HT-29	Growth Inhibition Assay			IC50=5.98118 μM	SANGER
SK-HEP-1	Growth Inhibition Assay			IC50=5.93471 μM	SANGER
NB10	Growth Inhibition Assay			IC50=5.8946 μM	SANGER
D-263MG	Growth Inhibition Assay			IC50=5.88351 μM	SANGER
SK-MES-1	Growth Inhibition Assay			IC50=5.83528 μM	SANGER
MEL-JUSO	Growth Inhibition Assay			IC50=5.7378 μM	SANGER
RERF-LC-MS	Growth Inhibition Assay			IC50=5.68803 μM	SANGER
TE-8	Growth Inhibition Assay			IC50=5.68537 μM	SANGER
RS4-11	Growth Inhibition Assay			IC50=5.66775 μM	SANGER
LU-99A	Growth Inhibition Assay			IC50=5.66451 μM	SANGER
PA-1	Growth Inhibition Assay			IC50=5.64265 μM	SANGER
HOS	Growth Inhibition Assay			IC50=5.62923 μM	SANGER
HuP-T3	Growth Inhibition Assay			IC50=5.62029 μM	SANGER
SW1710	Growth Inhibition Assay			IC50=5.61654 μM	SANGER
ME-180	Growth Inhibition Assay			IC50=5.58092 μM	SANGER
NBsusSR	Growth Inhibition Assay			IC50=5.57155 μM	SANGER
FADU	Growth Inhibition Assay			IC50=5.55726 μM	SANGER
Hs-578-T	Growth Inhibition Assay			IC50=5.53794 μM	SANGER
NUGC-3	Growth Inhibition Assay			IC50=5.49302 μM	SANGER
HCC2998	Growth Inhibition Assay			IC50=5.49109 μM	SANGER
GT3TKB	Growth Inhibition Assay			IC50=5.46598 μM	SANGER
NCI-H1155	Growth Inhibition Assay			IC50=5.40051 μM	SANGER
AsPC-1	Growth Inhibition Assay			IC50=5.36763 μM	SANGER
BCPAP	Growth Inhibition Assay			IC50=5.32969 μM	SANGER
HuH-7	Growth Inhibition Assay			IC50=5.27147 μM	SANGER
UM-UC-3	Growth Inhibition Assay			IC50=5.18047 μM	SANGER
23132-87	Growth Inhibition Assay			IC50=5.16872 μM	SANGER
CAL-33	Growth Inhibition Assay			IC50=5.12317 μM	SANGER
MOLT-13	Growth Inhibition Assay			IC50=5.06776 μM	SANGER
H4	Growth Inhibition Assay			IC50=5.04255 μM	SANGER
CAL-54	Growth Inhibition Assay			IC50=5.02695 μM	SANGER
EPLC-272H	Growth Inhibition Assay			IC50=4.99669 μM	SANGER
EFO-27	Growth Inhibition Assay			IC50=4.78667 μM	SANGER
LB1047-RCC	Growth Inhibition Assay			IC50=4.73815 μM	SANGER
NH-12	Growth Inhibition Assay			IC50=4.71625 μM	SANGER
NCI-H747	Growth Inhibition Assay			IC50=4.68807 μM	SANGER
NB5	Growth Inhibition Assay			IC50=4.60369 μM	SANGER
NCI-H358	Growth Inhibition Assay			IC50=4.45385 μM	SANGER
IGROV-1	Growth Inhibition Assay			IC50=4.45171 μM	SANGER
HH	Growth Inhibition Assay			IC50=4.41597 μM	SANGER
ALL-PO	Growth Inhibition Assay			IC50=4.36156 μM	SANGER
LAN-6	Growth Inhibition Assay			IC50=4.31637 μM	SANGER
MDA-MB-231	Growth Inhibition Assay			IC50=4.29223 μM	SANGER
HOP-92	Growth Inhibition Assay			IC50=4.2567 μM	SANGER
RPMI-7951	Growth Inhibition Assay			IC50=4.25589 μM	SANGER
MHH-PREB-1	Growth Inhibition Assay			IC50=4.12111 μM	SANGER
CAL-62	Growth Inhibition Assay			IC50=4.0743 μM	SANGER
SW626	Growth Inhibition Assay			IC50=4.0448 μM	SANGER
GAMG	Growth Inhibition Assay			IC50=4.02377 μM	SANGER
8505C	Growth Inhibition Assay			IC50=3.90078 μM	SANGER
CGTH-W-1	Growth Inhibition Assay			IC50=3.85725 μM	SANGER
SK-MEL-3	Growth Inhibition Assay			IC50=3.85154 μM	SANGER
NCI-H2087	Growth Inhibition Assay			IC50=3.84672 μM	SANGER
HPAF-II	Growth Inhibition Assay			IC50=3.7549 μM	SANGER
697	Growth Inhibition Assay			IC50=3.69603 μM	SANGER
SK-LU-1	Growth Inhibition Assay			IC50=3.68798 μM	SANGER
NCI-SNU-5	Growth Inhibition Assay			IC50=3.6773 μM	SANGER
U-2-OS	Growth Inhibition Assay			IC50=3.67256 μM	SANGER
EGI-1	Growth Inhibition Assay			IC50=3.60583 μM	SANGER
A427	Growth Inhibition Assay			IC50=3.59556 μM	SANGER
CTB-1	Growth Inhibition Assay			IC50=3.47047 μM	SANGER
PANC-03-27	Growth Inhibition Assay			IC50=3.35045 μM	SANGER
GAK	Growth Inhibition Assay			IC50=3.32561 μM	SANGER
786-0	Growth Inhibition Assay			IC50=3.27243 μM	SANGER
SN12C	Growth Inhibition Assay			IC50=3.24701 μM	SANGER
HSC-3	Growth Inhibition Assay			IC50=3.23151 μM	SANGER
COLO-741	Growth Inhibition Assay			IC50=3.18673 μM	SANGER
KU-19-19	Growth Inhibition Assay			IC50=3.17034 μM	SANGER
SW780	Growth Inhibition Assay			IC50=3.14229 μM	SANGER
LAMA-84	Growth Inhibition Assay			IC50=3.1358 μM	SANGER
D-423MG	Growth Inhibition Assay			IC50=3.07753 μM	SANGER
HT-1080	Growth Inhibition Assay			IC50=3.01997 μM	SANGER
MIA-PaCa-2	Growth Inhibition Assay			IC50=3.00781 μM	SANGER
Ca9-22	Growth Inhibition Assay			IC50=2.97255 μM	SANGER
NCI-H727	Growth Inhibition Assay			IC50=2.91796 μM	SANGER
T-24	Growth Inhibition Assay			IC50=2.91112 μM	SANGER
CAL-39	Growth Inhibition Assay			IC50=2.89999 μM	SANGER
LB2241-RCC	Growth Inhibition Assay			IC50=2.85893 μM	SANGER
COLO-792	Growth Inhibition Assay			IC50=2.84027 μM	SANGER
HCE-T	Growth Inhibition Assay			IC50=2.83264 μM	SANGER
BFTC-905	Growth Inhibition Assay			IC50=2.8253 μM	SANGER
CHL-1	Growth Inhibition Assay			IC50=2.80785 μM	SANGER
L-363	Growth Inhibition Assay			IC50=2.7437 μM	SANGER
HCC2218	Growth Inhibition Assay			IC50=2.64778 μM	SANGER
DB	Growth Inhibition Assay			IC50=2.58788 μM	SANGER
EW-13	Growth Inhibition Assay			IC50=2.56339 μM	SANGER
KNS-62	Growth Inhibition Assay			IC50=2.51164 μM	SANGER
RD	Growth Inhibition Assay			IC50=2.44723 μM	SANGER
BB65-RCC	Growth Inhibition Assay			IC50=2.40674 μM	SANGER
CAL-27	Growth Inhibition Assay			IC50=2.39236 μM	SANGER
DOK	Growth Inhibition Assay			IC50=2.35773 μM	SANGER
NB7	Growth Inhibition Assay			IC50=2.34086 μM	SANGER
A2058	Growth Inhibition Assay			IC50=2.19279 μM	SANGER
HN	Growth Inhibition Assay			IC50=2.16278 μM	SANGER
MZ2-MEL	Growth Inhibition Assay			IC50=2.11127 μM	SANGER
EM-2	Growth Inhibition Assay			IC50=2.07198 μM	SANGER
HCC70	Growth Inhibition Assay			IC50=2.02426 μM	SANGER
RXF393	Growth Inhibition Assay			IC50=1.97887 μM	SANGER
LCLC-97TM1	Growth Inhibition Assay			IC50=1.92256 μM	SANGER
A375	Growth Inhibition Assay			IC50=1.89714 μM	SANGER
BPH-1	Growth Inhibition Assay			IC50=1.89591 μM	SANGER
LOXIMVI	Growth Inhibition Assay			IC50=1.89427 μM	SANGER
NCI-H292	Growth Inhibition Assay			IC50=1.86699 μM	SANGER
NB69	Growth Inhibition Assay			IC50=1.78469 μM	SANGER
OVCAR-5	Growth Inhibition Assay			IC50=1.77687 μM	SANGER
COLO-829	Growth Inhibition Assay			IC50=1.62232 μM	SANGER
RT-112	Growth Inhibition Assay			IC50=1.58952 μM	SANGER
SK-MEL-2	Growth Inhibition Assay			IC50=1.57459 μM	SANGER
HD-MY-Z	Growth Inhibition Assay			IC50=1.57376 μM	SANGER
A4-Fuk	Growth Inhibition Assay			IC50=1.57045 μM	SANGER
SW1116	Growth Inhibition Assay			IC50=1.56398 μM	SANGER
NCI-H1437	Growth Inhibition Assay			IC50=1.55275 μM	SANGER
ML-2	Growth Inhibition Assay			IC50=1.52868 μM	SANGER
HO-1-N-1	Growth Inhibition Assay			IC50=1.51634 μM	SANGER
LoVo	Growth Inhibition Assay			IC50=1.46399 μM	SANGER
LS-513	Growth Inhibition Assay			IC50=1.45192 μM	SANGER
BV-173	Growth Inhibition Assay			IC50=1.44015 μM	SANGER
LS-411N	Growth Inhibition Assay			IC50=1.40517 μM	SANGER
SW1463	Growth Inhibition Assay			IC50=1.33721 μM	SANGER
NCI-H2291	Growth Inhibition Assay			IC50=1.32536 μM	SANGER
H-EMC-SS	Growth Inhibition Assay			IC50=1.29608 μM	SANGER
RCM-1	Growth Inhibition Assay			IC50=1.24047 μM	SANGER
SK-MEL-1	Growth Inhibition Assay			IC50=1.23419 μM	SANGER
ONS-76	Growth Inhibition Assay			IC50=1.22049 μM	SANGER
Mewo	Growth Inhibition Assay			IC50=1.20276 μM	SANGER
A549	Growth Inhibition Assay			IC50=1.19576 μM	SANGER
HuP-T4	Growth Inhibition Assay			IC50=1.18359 μM	SANGER
SW620	Growth Inhibition Assay			IC50=1.13534 μM	SANGER
SK-N-AS	Growth Inhibition Assay			IC50=1.07947 μM	SANGER
TYK-nu	Growth Inhibition Assay			IC50=1.03172 μM	SANGER
GP5d	Growth Inhibition Assay			IC50=0.98308 μM	SANGER
RVH-421	Growth Inhibition Assay			IC50=0.9718 μM	SANGER
UACC-257	Growth Inhibition Assay			IC50=0.96473 μM	SANGER
PSN1	Growth Inhibition Assay			IC50=0.96196 μM	SANGER
C2BBe1	Growth Inhibition Assay			IC50=0.81023 μM	SANGER
NCI-SNU-1	Growth Inhibition Assay			IC50=0.75433 μM	SANGER
LB2518-MEL	Growth Inhibition Assay			IC50=0.71632 μM	SANGER
HT-144	Growth Inhibition Assay			IC50=0.64657 μM	SANGER
HMV-II	Growth Inhibition Assay			IC50=0.64465 μM	SANGER
P12-ICHIKAWA	Growth Inhibition Assay			IC50=0.61221 μM	SANGER
A2780	Growth Inhibition Assay			IC50=0.49823 μM	SANGER
WM-115	Growth Inhibition Assay			IC50=0.49257 μM	SANGER
CP66-MEL	Growth Inhibition Assay			IC50=0.48809 μM	SANGER
HTC-C3	Growth Inhibition Assay			IC50=0.46531 μM	SANGER
SH-4	Growth Inhibition Assay			IC50=0.46256 μM	SANGER
KU812	Growth Inhibition Assay			IC50=0.45299 μM	SANGER
K5	Growth Inhibition Assay			IC50=0.43117 μM	SANGER
HL-60	Growth Inhibition Assay			IC50=0.41107 μM	SANGER
KASUMI-1	Growth Inhibition Assay			IC50=0.399 μM	SANGER
KY821	Growth Inhibition Assay			IC50=0.3791 μM	SANGER
G-361	Growth Inhibition Assay			IC50=0.36795 μM	SANGER
SK-MEL-24	Growth Inhibition Assay			IC50=0.32813 μM	SANGER
COLO-679	Growth Inhibition Assay			IC50=0.3272 μM	SANGER
KG-1	Growth Inhibition Assay			IC50=0.30668 μM	SANGER
SK-MEL-28	Growth Inhibition Assay			IC50=0.30409 μM	SANGER
BHT-101	Growth Inhibition Assay			IC50=0.28606 μM	SANGER
MEL-HO	Growth Inhibition Assay			IC50=0.27652 μM	SANGER
ACN	Growth Inhibition Assay			IC50=0.26737 μM	SANGER
MZ7-mel	Growth Inhibition Assay			IC50=0.2634 μM	SANGER
NOMO-1	Growth Inhibition Assay			IC50=0.25742 μM	SANGER
HSC-4	Growth Inhibition Assay			IC50=0.24395 μM	SANGER
KM12	Growth Inhibition Assay			IC50=0.24057 μM	SANGER
A101D	Growth Inhibition Assay			IC50=0.214 μM	SANGER
KMOE-2	Growth Inhibition Assay			IC50=0.19795 μM	SANGER
C32	Growth Inhibition Assay			IC50=0.19072 μM	SANGER
CP50-MEL-B	Growth Inhibition Assay			IC50=0.17254 μM	SANGER
M14	Growth Inhibition Assay			IC50=0.15468 μM	SANGER
AGS	Growth Inhibition Assay			IC50=0.11713 μM	SANGER
MMAC-SF	Growth Inhibition Assay			IC50=0.10974 μM	SANGER
DU-4475	Growth Inhibition Assay			IC50=0.07599 μM	SANGER
EoL-1-cell	Growth Inhibition Assay			IC50=0.04152 μM	SANGER
CHP-212	Growth Inhibition Assay			IC50=0.02885 μM	SANGER
H9	Growth Inhibition Assay			IC50=0.02276 μM	SANGER
HEL	Growth Inhibition Assay			IC50=24.0865 μM	SANGER
ABC-1	Growth Inhibition Assay			IC50=24.2729 μM	SANGER
COLO-680N	Growth Inhibition Assay			IC50=24.4764 μM	SANGER
MZ1-PC	Growth Inhibition Assay			IC50=24.687 μM	SANGER
NCI-H69	Growth Inhibition Assay			IC50=24.7354 μM	SANGER
TE-1	Growth Inhibition Assay			IC50=25.0499 μM	SANGER
EW-3	Growth Inhibition Assay			IC50=25.113 μM	SANGER
PANC-08-13	Growth Inhibition Assay			IC50=25.8103 μM	SANGER
NMC-G1	Growth Inhibition Assay			IC50=26.0088 μM	SANGER
BT-20	Growth Inhibition Assay			IC50=26.4543 μM	SANGER
TGBC24TKB	Growth Inhibition Assay			IC50=26.7331 μM	SANGER
TE-11	Growth Inhibition Assay			IC50=26.9895 μM	SANGER
ESS-1	Growth Inhibition Assay			IC50=27.3216 μM	SANGER
JVM-3	Growth Inhibition Assay			IC50=27.6475 μM	SANGER
C3A	Growth Inhibition Assay			IC50=27.8496 μM	SANGER
MDA-MB-157	Growth Inhibition Assay			IC50=27.8753 μM	SANGER
KLE	Growth Inhibition Assay			IC50=28.1058 μM	SANGER
ES1	Growth Inhibition Assay			IC50=28.1838 μM	SANGER
CAL-120	Growth Inhibition Assay			IC50=28.3999 μM	SANGER
NCI-N87	Growth Inhibition Assay			IC50=28.5105 μM	SANGER
RPMI-8226	Growth Inhibition Assay			IC50=29.1843 μM	SANGER
COR-L88	Growth Inhibition Assay			IC50=29.2419 μM	SANGER
UACC-893	Growth Inhibition Assay			IC50=29.3137 μM	SANGER
C8166	Growth Inhibition Assay			IC50=29.9996 μM	SANGER
J82	Growth Inhibition Assay			IC50=30.8147 μM	SANGER
PFSK-1	Growth Inhibition Assay			IC50=31.0659 μM	SANGER
COLO-684	Growth Inhibition Assay			IC50=31.4374 μM	SANGER
CAL-72	Growth Inhibition Assay			IC50=31.5729 μM	SANGER
SNB75	Growth Inhibition Assay			IC50=31.897 μM	SANGER
MDA-MB-415	Growth Inhibition Assay			IC50=31.9762 μM	SANGER
SiHa	Growth Inhibition Assay			IC50=32.4711 μM	SANGER
NCI-H1648	Growth Inhibition Assay			IC50=32.9345 μM	SANGER
EFO-21	Growth Inhibition Assay			IC50=33.005 μM	SANGER
HCC38	Growth Inhibition Assay			IC50=33.3841 μM	SANGER
IA-LM	Growth Inhibition Assay			IC50=33.7889 μM	SANGER
CTV-1	Growth Inhibition Assay			IC50=33.9786 μM	SANGER
NCI-H446	Growth Inhibition Assay			IC50=34.2689 μM	SANGER
IST-SL1	Growth Inhibition Assay			IC50=34.7408 μM	SANGER
EW-22	Growth Inhibition Assay			IC50=34.7759 μM	SANGER
JEG-3	Growth Inhibition Assay			IC50=36.1766 μM	SANGER
LU-65	Growth Inhibition Assay			IC50=36.2985 μM	SANGER
NCI-H596	Growth Inhibition Assay			IC50=36.9591 μM	SANGER
KNS-81-FD	Growth Inhibition Assay			IC50=37.145 μM	SANGER
NCI-H1793	Growth Inhibition Assay			IC50=37.7086 μM	SANGER
NCI-H460	Growth Inhibition Assay			IC50=38.0873 μM	SANGER
MPP-89	Growth Inhibition Assay			IC50=39.5886 μM	SANGER
D-542MG	Growth Inhibition Assay			IC50=39.8436 μM	SANGER
JAR	Growth Inhibition Assay			IC50=40.4705 μM	SANGER
NCI-H209	Growth Inhibition Assay			IC50=40.677 μM	SANGER
G-402	Growth Inhibition Assay			IC50=41.3993 μM	SANGER
IST-MES1	Growth Inhibition Assay			IC50=42.1935 μM	SANGER
Daoy	Growth Inhibition Assay			IC50=42.5471 μM	SANGER
EW-11	Growth Inhibition Assay			IC50=43.1211 μM	SANGER
Saos-2	Growth Inhibition Assay			IC50=43.1537 μM	SANGER
no-10	Growth Inhibition Assay			IC50=43.1702 μM	SANGER
HCC1395	Growth Inhibition Assay			IC50=43.4644 μM	SANGER
HCE-4	Growth Inhibition Assay			IC50=43.7664 μM	SANGER
EW-1	Growth Inhibition Assay			IC50=43.8049 μM	SANGER
OCUB-M	Growth Inhibition Assay			IC50=44.3638 μM	SANGER
IGR-1	Growth Inhibition Assay			IC50=44.4115 μM	SANGER
NCI-H1838	Growth Inhibition Assay			IC50=44.4349 μM	SANGER
NCI-H2405	Growth Inhibition Assay			IC50=44.534 μM	SANGER
GB-1	Growth Inhibition Assay			IC50=44.7463 μM	SANGER
MG-63	Growth Inhibition Assay			IC50=46.0696 μM	SANGER
KP-N-YN	Growth Inhibition Assay			IC50=46.4679 μM	SANGER
no-11	Growth Inhibition Assay			IC50=47.0244 μM	SANGER
SW948	Growth Inhibition Assay			IC50=47.3377 μM	SANGER
CAMA-1	Growth Inhibition Assay			IC50=47.3438 μM	SANGER
HCC1187	Growth Inhibition Assay			IC50=47.51 μM	SANGER
D-392MG	Growth Inhibition Assay			IC50=47.6516 μM	SANGER
647-V	Growth Inhibition Assay			IC50=49.3414 μM	SANGER
HeLa	Function assay			Concentration-dependent inhibition of ERK5 phosphorylation shift in EGF-stimulated HeLa cells	17850214
HeLa	Function assay			Concentration-dependent inhibition of ERK1, ERK2 phosphorylation in EGF-stimulated HeLa cells	17850214
Colon 26	Function assay			Inhibition of MEK in mouse colon 26 carcinoma cells assessed as inhibition of ERK phosphorylation by ELISA, IC50=0.046μM	17880056
Colon 26	Function assay			Inhibition of MEK in mouse Colon 26 cells by Western blot, IC50=0.053μM	18951019
K-Balb	Function assay		1 hr	Inhibition of MEK-mediated ERK phosphorylation in PDGF-stimulated mouse K-Balb cells treated as single oral dose preincubated for 1 hr before PDGF challenge by whole cell assay, IC50=0.00245μM	18952427
C26	Function assay			Inhibition of MEK-stimulated ERK phosphorylation in PDGF-stimulated mouse C26 cells treated as single oral dose before PDGF challenge by whole cell assay, IC50=0.0035μM	18952427
K-Balb	Function assay		24 hrs	Inhibition of MEK-mediated ERK phosphorylation in PDGF-stimulated mouse K-Balb cells treated as single oral dose preincubated for 24 hrs before PDGF challenge by whole cell assay, IC50=0.0354μM	18952427
U937	Cytotoxicity assay	30 uM		Cytotoxicity against human U937 cells assessed as inhibition of [3H]thymidine incorporation at 30 uM by MTS assay	20580230
U937	Function assay	3 uM		Inhibition of ERK phosphorylation in human U937 cells at 3 uM by Western blotting	20580230
U937	Function assay	3 uM		Inhibition of RSK1 phosphorylation in human U937 cells at 3 uM by Western blotting	20580230
U937	Cytotoxicity assay	10 uM		Cytotoxicity against human U937 cells assessed as cell death at 10 uM by 7-AAD assay	20580230
U937	Cell cycle assay		24 hrs	Cell cycle arrest in human U937 cells assessed as decrease in S-phase population after 24 hrs by propidium iodide staining-based flow cytometric analysis in presence of MEK inhibitor PD184352	22074985
U937	Cell cycle assay		24 hrs	Cell cycle arrest in human U937 cells assessed as accumulation at G2/M-phase after 24 hrs by propidium iodide staining-based flow cytometric analysis in presence of MEK inhibitor PD184352	22074985
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
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
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
786-0	Function assay		24 hrs	Inhibition of CK2 in human 786-0 cells assessed as decrease in Akt1 phosphorylation at Ser129 after 24 hrs by Western blot analysis, EC50=0.1μM	30689946
Haga clic para ver más datos experimentales de líneas celulares

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	478.67	Fórmula	C₁₇H₁₄ClF₂IN₂O₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	212631-79-3	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	C1CC1CONC(=O)C2=C(C(=C(C=C2)F)F)NC3=C(C=C(C=C3)I)Cl

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 96 mg/mL (200.55 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Ethanol : 14 mg/mL

Water : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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.
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	30%PEG400 1 0.5%Tween80 2 5%propylene glycol, pH 9 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	10.000mg/ml (20.89mM)	Taking the 1 mL working solution as an example, add 300 μL of 33.33 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol, pH 9, to the above system, mix evenly to clarify it; then continue Add 645 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Características	First MEK inhibitor to begin clinical development.
Targets/IC₅₀/Ki	MEK1 (Cell-free assay) 17 nM MEK2 (Cell-free assay) 17 nM
In vitro	El tratamiento con CI-1040 produce una reducción de los niveles de pMAPK en múltiples células tumorales, incluyendo carcinomas de colon 26, pancreáticos BX-PC3, cervicales A431, colon HT-29, mama ZR-25-1 y ováricos SKOV-3. Este tratamiento no inhibe la fosforilación de Jun quinasa, p38 quinasa o Akt, lo que indica que se dirige específicamente a MEK. La inhibición de la activación de MAPK por esta sustancia química previene la progresión del ciclo celular e induce un bloqueo en G1. La IC50 para la inhibición de MEK1 por este inhibidor es de 0,3 μM, 15 veces mayor que la concentración requerida para inhibir la activación de ERK2 inducida por EGF en células Swiss 3T3. Estos resultados indican que este agente ejerce sus efectos sobre las células suprimiendo la activación de MKK1, y no bloqueando su actividad. 2 nM de este compuesto inhiben la activación de MKK1 en células Swiss 3T3 en un 50%, mientras que una concentración más de 100 veces superior inhibe MEK1 in vitro. También inhibe la fosforilación de MEK1 catalizada por Raf sin ningún efecto sobre la fosforilación de la proteína básica de mielina catalizada por Raf. Este químico inhibe el 86% del crecimiento de células de carcinoma papilar de tiroides (CPT) con el reordenamiento RET/PTC1 a 10 μM en comparación con las células tratadas solo con DMSO. Muestra una potente inhibición de las células CPT (mutación BRAF) con una GI50 de 52 nM, pero baja actividad en el tipo de reordenamiento RET/PTC1 con una GI50 de 1,1 μM. Una investigación reciente indica que este agente aumenta el efecto apoptótico de BMS-214662 en una línea celular de crisis blástica de LMC, K562, y en células primarias de LMC CD34+ en fase crónica.
Ensayo de quinasa	Ensayo de MEK1
Ensayo de quinasa	La cinasa MAP se activa después de la fosforilación por MEK; la cinasa MAP activada fosforila posteriormente la proteína básica de la mielina (MBP). La incorporación de ³²P en la proteína básica de la mielina (MBP) se ensaya en presencia de proteínas de fusión de glutatión S-transferasa (GST) que contienen la MAPK de 44 kDa (GST-MAPK) o la MEK de 45 kDa (GST-MEK1). Los ensayos se realizan en 50 μL de 50 mM Tris, pH 7,4/10 mM MgCl₂ /2 mM EGTA/10 μM [γ-³²P]ATP que contienen 10 μg de GST-MEK1, 0,5 μg de GST-MAPK y 40 μg de MBP. Después de la incubación a 30 °C durante 15 minutos, las reacciones se detienen mediante la adición de tampón de muestra Laemmli SDS. La MBP fosforilada se resuelve mediante SDS/PAGE al 10%. Este esfuerzo de cribado conduce al descubrimiento de varios inhibidores de moléculas pequeñas de MEK, es decir, PD184352 (CI-1040). Experimentos que evalúan el orden de adición muestran que este compuesto inhibe directamente MEK1 con una concentración inhibitoria del 50 % (IC50) de 17 nM, sin afectar la actividad de MAPK.
In vivo	La administración oral de CI-1040 deteriora el crecimiento de xenoinjertos de tumores de colon de ratón y humanos con un amplio rango de dosis de 48-200 mg/kg por dosis, pero no de la leucemia P388. Este compuesto inhibe los xenoinjertos tumorales de células de CPT que portan una mutación BRAF con una reducción del 31,3%, y que portan el reordenamiento RET/PTC1 con una reducción del 47,5% que en ratones no tratados (vehículo) después de 3 semanas de administración oral (300 mg/kg/día). No se observan efectos tóxicos en ninguno de los ratones cuando se tratan con este químico. La exposición transitoria de tumores mamarios a este compuesto y a UCN-01 provoca la muerte de células tumorales in vivo y una supresión prolongada del recrecimiento tumoral. El tratamiento combinado con este químico (25 mg/kg) y UCN-01 (0,1-0,2 mg/kg) reduce significativamente MDA-MB-231, y en gran medida suprime el crecimiento tumoral de MCF7 en ratones atímicos implantados, mientras que cualquiera de los tratamientos individuales no tiene una actividad significativa. La combinación de fármacos conduce a una profunda muerte de células tumorales que se correlaciona con una reducción en la fosforilación de ERK1/2 y la inmunorreactividad de Ki67 y de CD31.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/10395327/ [2] https://pubmed.ncbi.nlm.nih.gov/10998351/ [3] https://pubmed.ncbi.nlm.nih.gov/19380355/ [4] https://pubmed.ncbi.nlm.nih.gov/21483442/ [5] https://pubmed.ncbi.nlm.nih.gov/16319524/ [6] https://pubmed.ncbi.nlm.nih.gov/18056456/ [7] https://pubmed.ncbi.nlm.nih.gov/19737956/ [8] https://pubmed.ncbi.nlm.nih.gov/17363501/

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	p-ERK5 / ERK5 p-ERK1/2 / ERK1/2		21762482
Growth inhibition assay	Cell viability		29989268

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):