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PI-103 PI3K inhibidor

Name: PI-103
Brand: Selleck Chemicals
SKU: S1038
Rating: 5 (104 reviews)

Cat. No.S1038

PI-103 es un inhibidor de PI3K multidirigido para p110α/β/δ/γ con IC50 de 2 nM/3 nM/3 nM/15 nM en ensayos sin células, menos potente para mTOR/DNA-PK con IC50 de 30 nM/23 nM. Este compuesto induce apoptosis en linfoma murino de células T.

PI-103 PI3K inhibidor Chemical Structure

Estructura química

Peso molecular: 348.36

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Control de calidad

Lote: Pureza: 99.59%

99.59

Dianas relacionadas	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Otros PI3K Inhibidores	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) LY294002 XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549)

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Formulación	Descripción de la actividad	PMID
UCH-1	Apoptosis Assay	0.1-10 μM	24 h	DMSO	induces apoptosis	19528441
UCH-1	Growth Inhibition Assay	0.01-10 μM	6 d		inhibits proliferation dose dependently	19528441
UCH-1	Function Assay	0-5 μM			inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner	19528441
HUVEC	Growth Inhibition Assay				IC50=0.08 μM	19584227
SKOV-3	Growth Inhibition Assay				IC50=0.12 μM	19584227
PC3	Growth Inhibition Assay				IC50=0.10 μM	19584227
DETROIT562	Growth Inhibition Assay				IC50=0.13 μM	19584227
IGROV-1	Growth Inhibition Assay				IC50=0.06 μM	19584227
U87MG	Growth Inhibition Assay				IC50=0.14 μM	19584227
U118MG	Function Assay	0.1-1 μM	24 h	DMSO	inhibits PI3K-mediated signaling	19633683
U138MG	Function Assay	0.1-1 μM	24 h	DMSO	inhibits PI3K-mediated signaling	19633683
U87MG	Function Assay	0.1-1 μM	24 h	DMSO	inhibits PI3K-mediated signaling	19633683
PC3	Growth Inhibition Assay		24h		GI50 = 100 nM	20551061
518A2	Function Assay	0.001–1 μM	24 h		suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
Mel-Juso	Function Assay	0.001–1 μM	24 h		suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
518A2	Cell Viability Assay	0.01–10 μM	72 h		inhibits cell viability dose dependently	21048785
Mel-Juso	Cell Viability Assay	0.01–10 μM	72 h		inhibits cell viability dose dependently	21048785
SF767	Function Assay	1 μM	48 h		induces autophagosome formation	21062993
U373	Function Assay	1 μM	48 h		induces autophagosome formation	21062993
U87	Function Assay	1 μM	48 h		induces autophagosome formation	21062993
LN229	Function Assay	1 μM	48 h		induces autophagosome formation	21062993
PC-9	Growth Inhibition Assay	0-3 μM	72 h		IC50=0.8 μM	21220474
HCC827	Growth Inhibition Assay	0-3 μM	72 h		IC50=0.3 μM	21220474
HCC1937	Function Assay	1 μM	24 h		reduces the phosphorylation of AKT	22488590
SUM1315MO2	Function Assay	1 μM	24 h		reduces the phosphorylation of AKT	22488590
SUM149PT	Function Assay	1 μM	24 h		reduces the phosphorylation of AKT	22488590
MDA-MB-436	Function Assay	1 μM	24 h		reduces the phosphorylation of AKT	22488590
KMS12-BM	Growth Inhibition Assay	0-2 μM	24 h		IC50＞2 μM	22829234
NCI-H929	Growth Inhibition Assay	0-2 μM	24 h		IC50=0.25 μM	22829234
MM1S	Growth Inhibition Assay	0-2 μM	24 h		IC50=0.5 μM	22829234
MOLT-16	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
LOUCY	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
CCRF-CEM	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
PF-382	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
MOLT-4	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
Jurkat	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
RPMI-8402	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
Karpas-45	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
KE37	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
ALL-SIL	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
PEER	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
SUP-T1	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
DND41	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
HPB-ALL	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
TALL-1	Growth Inhibition Assay	1 μM	7 d		decreases the cell number significantly	23038273
H3122	Function Assay	0-3.3 μM	72 h		induces complete downregulation of pAKT	23259591
HCC827	Function Assay	0-3.3 μM	72 h		induces complete downregulation of pAKT	23259591
A549	Function Assay	0-3.3 μM	72 h		induces complete downregulation of pAKT	23259591
HT1080	Apoptosis Assay	3 µM	12 h	DMSO	sensitizes RD cells to DOX-induced apoptosis	23300809
TP5014	Apoptosis Assay	3 µM	12 h	DMSO	sensitizes RD cells to DOX-induced apoptosis	23300809
RD	Apoptosis Assay	3 µM	12 h	DMSO	sensitizes RD cells to DOX-induced apoptosis	23300809
SKNBE(2c)	Function Assay	1.5/2.5/5 μM	24 h		induces G1 cell-cycle arrest and apoptosis	23378341
SY5Y	Function Assay	1.5/2.5/5 μM	24 h		induces G1 cell-cycle arrest and apoptosis	23378341
MDA-MB-231	Cell Viability Assay	0.3 μM	72 h		enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
MDA-MB-468	Cell Viability Assay	0.3 μM	72 h		enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
SUM149PT	Cell Viability Assay	0.3 μM	72 h		enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
RMS13	Apoptosis Assay	1/1.5/2 μM	72 h	DMSO	induces caspase-dependent apoptosis combined with UO126	23684925
RH30	Apoptosis Assay	1/1.5/2 μM	72 h	DMSO	induces caspase-dependent apoptosis combined with UO126	23684925
TE671	Apoptosis Assay	1/1.5/2 μM	72 h	DMSO	induces caspase-dependent apoptosis combined with UO126	23684925
RD	Apoptosis Assay	1/1.5/2 μM	72 h	DMSO	induces caspase-dependent apoptosis combined with UO126	23684925
FaDu	Function Assay	0.25/0.5/1 μM	24 h		inhibits Akt phosphorylation significantly	24351425
UT5	Function Assay	0.25/0.5/1 μM	24 h		inhibits Akt phosphorylation significantly	24351425
SAS	Function Assay	0.25/0.5/1 μM	24 h		inhibits Akt phosphorylation significantly	24351425
H661	Function Assay	0.25/0.5/1 μM	24 h		inhibits Akt phosphorylation significantly	24351425
H460	Function Assay	0.25/0.5/1 μM	24 h		inhibits Akt phosphorylation slightly	24351425
A549	Function Assay	0.25/0.5/1 μM	24 h		inhibits Akt phosphorylation slightly	24351425
NUGC4 LG	Growth Inhibition Assay				IC50=14.0 ± 5.321 μM	24597478
NUGC4 HG	Growth Inhibition Assay				IC50=14.0 ± 3.913 μM	24597478
MKN45 LG	Growth Inhibition Assay				IC50=0.87 ± 0.030 μM	24597478
MKN45 HG	Growth Inhibition Assay				IC50=1.01 ± 0.051 μM	24597478
HGC27 LG	Growth Inhibition Assay				IC50=0.02 ± 0.004 μM	24597478
HGC27 HG	Growth Inhibition Assay				IC50=0.38 ± 0.022 μM	24597478
AGS LG	Growth Inhibition Assay				IC50=0.05 ± 0.001 μM	24597478
AGS HG	Growth Inhibition Assay				IC50=0.68 ± 0.031 μM	24597478
SW982	Apoptosis Assay	0.01-0.5 μM	48 h		induces apoptosis dose dependently	24695632
SW872	Apoptosis Assay	0.01-0.5 μM	48 h		induces apoptosis dose dependently	24695632
SW982	Function Assay	0.01-0.5 μM	24 h		reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner	24695632
SW872	Function Assay	0.01-0.5 μM	24 h		reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner	24695632
HS578T	Function Assay	0.01-10 μM	24 h		downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
MDA-MB-231	Function Assay	0.01-10 μM	24 h		downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
MDA-MB-468	Function Assay	0.01-10 μM	24 h		downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins	25721419
SUM149PT	Cell Viability Assay	0-3 μM	72 h		inhibits cell viability dose dependently	25721419
MDA-MB-436	Cell Viability Assay	0-3 μM	72 h		inhibits cell viability dose dependently	25721419
MDA-MB-468	Cell Viability Assay	0-3 μM	72 h		inhibits cell viability dose dependently	25721419
MDA-MB-231	Cell Viability Assay	0-3 μM	72 h		inhibits cell viability dose dependently	25721419
BT549	Cell Viability Assay	0-3 μM	72 h		inhibits cell viability dose dependently	25721419
HS578T	Cell Viability Assay	0-3 μM	72 h		inhibits cell viability dose dependently	25721419
VJ	Apoptosis Assay	1/1.5/2 μM	72 h		induces apoptosis combined with GANT61	25749378
RH30	Apoptosis Assay	1/1.5/2 μM	72 h		induces apoptosis combined with GANT61	25749378
RMS13	Apoptosis Assay	1/1.5/2 μM	72 h		induces apoptosis combined with GANT61	25749378
TE381.T	Apoptosis Assay	1/1.5/2 μM	72 h		induces apoptosis combined with GANT61	25749378
RD	Apoptosis Assay	1/1.5/2 μM	72 h		induces apoptosis combined with GANT61	25749378
G 40 DC	Growth Inhibition Assay	0.05-20 μM	24/72 h	DMSO	inhibits cell viability dose and time dependently	26121251
G 38 DC	Growth Inhibition Assay	0.05-20 μM	24/72 h	DMSO	inhibits cell viability dose and time dependently	26121251
G 35 DC	Growth Inhibition Assay	0.05-20 μM	24/72 h	DMSO	inhibits cell viability dose and time dependently	26121251
G 40 SC	Growth Inhibition Assay	0.05-20 μM	24/72 h	DMSO	inhibits cell viability dose and time dependently	26121251
G 38 SC	Growth Inhibition Assay	0.05-20 μM	24/72 h	DMSO	inhibits cell viability dose and time dependently	26121251
G 35 SC	Growth Inhibition Assay	0.05-20 μM	24/72 h	DMSO	inhibits cell viability dose and time dependently	26121251
SH-SY5Y	Apoptosis Assay	1 μM	0.5-24 h		sensitizes neuroblastoma cells to doxorubicin-induced apoptosis	26224681
SH-SY5Y	Growth Inhibition Assay	0-8 μM	24/48/72 h		induces time- and concentration-dependent inhibition on NB cell growth	26224681
SK-N-BE	Growth Inhibition Assay	0-8 μM	24/48/72 h		induces time- and concentration-dependent inhibition on NB cell growth	26224681
TT	Antiproliferative assay		13 days		Antiproliferative activity against human TT cells after 13 days by fluorescence assay, IC50=0.0022μM.	18849971
Sf9	Function assay		30 mins		Inhibition of N-terminal His-6-tagged full length human PI3Kalpha expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=0.0179μM.	24900786
HEK293T	Function assay		15 mins		Inhibition of mTORC1 (unknown origin) expressed in HEK293T cells after 15 mins in presence of gamma-[32]P-ATP by high-throughput screening assay, IC50=0.02μM.	29211480
Sf9	Function assay		30 mins		Inhibition of GST-tagged full length human PI3Kalpha D810A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=0.074μM.	24900786
Sf9	Function assay		30 mins		Inhibition of GST-tagged full length human PI3Kalpha Y836A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=0.7963μM.	24900786
Caco2	Antiproliferative assay		48 hrs		Antiproliferative activity against human Caco2 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=0.8μM.	30655216
Caco2	Antiproliferative assay		48 hrs		Antiproliferative activity against human Caco2 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=0.9μM.	23063566
HCT116	Antiproliferative assay		48 hrs		Antiproliferative activity against human HCT116 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=1μM.	23063566
Sf9	Function assay		30 mins		Inhibition of GST-tagged full length human PI3Kalpha M772A mutant expressed in baculovirus-infected sf9 cells after 30 mins by TR-FRET assay, IC50=1.0344μM.	24900786
PC3	Antiproliferative assay		48 hrs		Antiproliferative activity against human PC3 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=1.2μM.	30655216
HuH7	Antiproliferative assay		48 hrs		Antiproliferative activity against human HuH7 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=1.5μM.	23063566
PC3	Antiproliferative assay		48 hrs		Antiproliferative activity against human PC3 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=1.5μM.	23063566
Caco2	Cytotoxicity assay		48 hrs		Cytotoxicity against human Caco2 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=2μM.	28214231
HaCaT	Antiproliferative assay		48 hrs		Antiproliferative activity against human HaCaT cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=2μM.	30655216
NCI-H727	Antiproliferative assay		48 hrs		Antiproliferative activity against human NCI-H727 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=3μM.	23063566
MCF7	Cytotoxicity assay		48 hrs		Cytotoxicity against human MCF7 cells measured after 48 hrs by MTT assay, IC50=3μM.	28011424
HCT116	Antiproliferative assay		48 hrs		Antiproliferative activity against human HCT116 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=3μM.	30655216
HaCaT	Cytotoxicity assay		48 hrs		Cytotoxicity against human HaCaT cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=3.5μM.	28214231
HCT116	Cytotoxicity assay		48 hrs		Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=3.9μM.	28214231
A549	Cytotoxicity assay		48 hrs		Cytotoxicity against human A549 cells measured after 48 hrs by MTT assay, IC50=4μM.	28011424
MIAPaCa2	Cytotoxicity assay		48 hrs		Cytotoxicity against human MIAPaCa2 cells measured after 48 hrs by MTT assay, IC50=6μM.	28011424
HuH7	Antiproliferative assay		48 hrs		Antiproliferative activity against human HuH7 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=6μM.	30655216
ECV304	Antiproliferative assay				Antiproliferative activity against human ECV304 cells, IC50=6.3μM.	22130133
Bel7404	Antiproliferative assay				Antiproliferative activity against human Bel7404 cells, IC50=7μM.	22130133
PC3	Cytotoxicity assay		48 hrs		Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by Hoechst 33342 staining based assay, IC50=7.6μM.	28214231
HepG2	Cytotoxicity assay		48 hrs		Cytotoxicity against human HepG2 cells measured after 48 hrs by MTT assay, IC50=8μM.	28011424
MDA-MB-231	Antiproliferative assay		48 hrs		Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by Hoechst 33342 staining-based assay, IC50=8μM.	30655216
MDA-MB-231	Antiproliferative assay		48 hrs		Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by Hoechst 3342 dye staining based assay, IC50=15μM.	23063566
MCF7	Antiproliferative assay				Antiproliferative activity against human MCF7 cells, IC50=22.4μM.	22130133
HEK293	Function assay	0.5uM			Inhibition of PKB-S473 phosphorylation in IGF-1 treated HEK293 cells at 0.5uM	17850214
U87	Antiproliferative assay	0.04 to 10 uM	72 hrs		Antiproliferative activity against human U87 cells harboring mutations in PI(3)K pathway components at 0.04 to 10 uM after 72 hrs by fluorescence assay	18849971
LN229	Antiproliferative assay	0.04 to 10 uM	72 hrs		Antiproliferative activity against human LN229 cells harboring mutations in PI(3)K pathway components at 0.04 to 10 uM after 72 hrs by fluorescence assay	18849971
U87	Cell cycle assay	2.5 uM	24 hrs		Cell cycle arrest in human U87 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis	18849971
LN229	Cell cycle assay	2.5 uM	24 hrs		Cell cycle arrest in human LN229 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis	18849971
SEG1	Cell cycle assay	2.5 uM	24 hrs		Cell cycle arrest in human SEG1 cells assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis	18849971
TT	Function assay	0.04 to 10 uM	2 hrs		Inhibition of S6K autophosphorylation in human TT cells at 0.04 to 10 uM after 2 hrs by Western blot analysis	18849971
K562	Cell cycle assay	2.5 uM	24 hrs		Cell cycle arrest in human K562 cells harboring Bcr/Abl gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis	18849971
K562	Cell cycle assay	2.5 uM	24 hrs		Cell cycle arrest in human K562 cells harboring Bcr/Abl T315I mutant gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis	18849971
BA/F3	Cell cycle assay	2.5 uM	24 hrs		Cell cycle arrest in mouse BA/F3 cells harboring Bcr/Abl gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis	18849971
BA/F3	Cell cycle assay	2.5 uM	24 hrs		Cell cycle arrest in mouse BA/F3 cells harboring Bcr/Abl T315I mutant gene assessed as accumulation at G0/G1 phase at 2.5 uM after 24 hrs by FACS analysis	18849971
Rh30	Cell cycle assay	1 to 10 uM			Cell cycle arrest in human Rh30 cells assessed as increase in G1 cell population at 1 to 10 uM by flow cytometric analysis	22130133
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
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
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
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
Rh30	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
LAN-5	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 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
SJ-GBM2	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 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
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 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
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 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
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 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
Caco2	Cell cycle assay				Cell cycle arrest in human Caco2 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HCT116	Cell cycle assay				Cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase by Hoechst staining based fluorescence assay	28214231
PC3	Cell cycle assay				Cell cycle arrest in human PC3 cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
HaCaT	Cell cycle assay				Cell cycle arrest in human HaCaT cells assessed as accumulation at G1/S phase by Hoechst staining based fluorescence assay	28214231
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Información química, almacenamiento y estabilidad

Peso molecular	348.36	Fórmula	C₁₉H₁₆N₄O₃	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	371935-74-9	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	N/A			Smiles	C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

Solubilidad

In vitro
Lote:

DMSO : 24 mg/mL (68.89 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.000mg/ml (2.87mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 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.

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

Características	The first potent, synthetic mTOR inhibitor.
Targets/IC₅₀/Ki	p110α (Cell-free assay) 2 nM p110β (Cell-free assay) 3 nM p110δ (Cell-free assay) 3 nM p110γ (Cell-free assay) 15 nM DNA-PK (Cell-free assay) 23 nM mTOR (Cell-free assay) 30 nM
In vitro	PI-103 inhibe potentemente tanto los complejos de la proteína quinasa mTOR sensibles (mTORC1) como los insensibles (mTORC2) a la rapamicina. Este compuesto inhibe la activación constitutiva e inducida por factores de crecimiento de PI3K/Akt, así como la activación de mTORC1. En las células blásticas, inhibe la proliferación leucémica, la clonogenicidad de los progenitores leucémicos e induce la apoptosis mitocondrial, especialmente en el compartimento que contiene las células madre leucémicas. Este químico inhibe p110α >200 veces más potentemente que p110β. También bloquea potentemente la producción de PI(3,4)P2 y PIP3 en adipocitos y PIP3 en miotubos. Este compuesto inhibe la fosforilación de Akt con un IC95 100 veces menor que el de LY294002. Sorprendentemente, protege completamente a los animales de la disminución estimulada de la glucosa en sangre. Tiene efectos proapoptóticos aditivos en células blásticas y en células leucémicas inmaduras.
Ensayo de quinasa	Ensayos enzimáticos
Ensayo de quinasa	La actividad inhibidora de la fosfatidilinositol 3-quinasa se determinó utilizando un ensayo de proximidad por centelleo en presencia de 1 μmol/L de ATP. La inhibición de la proteína quinasa mTOR se determinó utilizando un método LanthaScreen basado en TR-FRET de Invitrogen. Este compuesto se ensayó a una concentración máxima de 10 μmol/L en presencia de 1 μmol/L de ATP, y los valores de IC50 se determinaron utilizando el software GraphPad Prism.
In vivo	Cuando los tumores alcanzan los 50-100 mm³, los animales se aleatorizan y se tratan con vehículo o PI-103. Este compuesto exhibe una actividad significativa, disminuyendo el tamaño promedio del tumor en 4 veces después de 18 días. Los ratones tratados con este químico no muestran signos obvios de toxicidad premórbida (basado en el peso corporal, la ingesta de alimentos y agua, la actividad y el examen general) o en la necropsia. Los tumores tratados muestran niveles disminuidos de Akt y S6 fosforilados, consistente con el bloqueo de p110α y mTOR. Este tratamiento es citostático para los xenoinjertos de glioma.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/16647110/ [2] https://pubmed.ncbi.nlm.nih.gov/16697955/ [3] https://pubmed.ncbi.nlm.nih.gov/19584227/

Aplicaciones

Métodos	Biomarcadores	PMID
Western blot	β-TrCP1 / p-mTOR p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38	25721419
Immunofluorescence	autophagosomes / autolysosomes	26814436
Growth inhibition assay	Cell viability	25721419

Soporte técnico

Instrucciones de manipulación

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