pour la recherche uniquement

PI-103 Inhibiteur de PI3K

Name: PI-103
Brand: Selleck Chemicals
SKU: S1038
Rating: 5 (105 reviews)

Réf. Catalogue: S1038

PI-103 est un inhibiteur de PI3K multi-cibles pour p110α/β/δ/γ avec des IC50 de 2 nM/3 nM/3 nM/15 nM dans les essais sans cellules, moins puissant pour mTOR/DNA-PK avec des IC50 de 30 nM/23 nM. Ce composé induit l'apoptose dans le lymphome murin à cellules T.

PI-103 PI3K Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 348.36

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.59%

99.59

Cibles apparentées	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Autre PI3K Inhibiteurs	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)

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Formulation	Description de l'activité	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
Cliquez pour voir plus de données expérimentales sur la lignée cellulaire

Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	348.36	Formule	C₁₉H₁₆N₄O₃	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	371935-74-9	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			Smiles	C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

Solubilité (Solubility)

In vitro
Lot:

DMSO : 24 mg/mL (68.89 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : 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 d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

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

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y 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 d'abord 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, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

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

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (Mechanism of Action)

Caractéristiques	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 puissamment les complexes de la protéine kinase mTOR sensibles (mTORC1) et insensibles (mTORC2) à la rapamycine. Ce composé inhibe l'activation constitutive et induite par les facteurs de croissance de PI3K/Akt, ainsi que l'activation de mTORC1. Dans les cellules blastiques, il inhibe la prolifération leucémique, la clonogénicité des progéniteurs leucémiques et induit l'apoptose mitochondriale, en particulier dans le compartiment contenant les cellules souches leucémiques. Ce produit chimique inhibe p110α plus de 200 fois plus puissamment que p110β. Il bloque également puissamment la production de PI(3,4)P2 et de PIP3 dans les adipocytes et de PIP3 dans les myotubes. Ce composé inhibe la phosphorylation d'Akt avec une IC95 100 fois inférieure à celle du LY294002. De manière frappante, il protège complètement les animaux d'une baisse stimulée de la glycémie. Il a des effets proapoptotiques additifs dans les cellules blastiques et dans les cellules leucémiques immatures.
Essai kinase	Essais enzymatiques
Essai kinase	L'activité inhibitrice de la phosphatidylinositide 3-kinase a été déterminée en utilisant un essai de scintillation de proximité en présence de 1 μmol/L d'ATP. L'inhibition de la protéine kinase mTOR a été déterminée en utilisant une méthode LanthaScreen basée sur le TR-FRET d'Invitrogen. Ce composé a été testé à une concentration maximale de 10 μmol/L en présence de 1 μmol/L d'ATP, et les valeurs d'IC50 ont été déterminées à l'aide du logiciel GraphPad Prism.
In vivo	Lorsque les tumeurs atteignent 50-100 mm³, les animaux sont randomisés et traités avec le véhicule ou PI-103. Ce composé présente une activité significative, diminuant la taille moyenne des tumeurs d'un facteur 4 après 18 jours. Les souris traitées avec ce produit chimique ne présentent aucun signe évident de toxicité avant la maladie (basé sur le poids corporel, l'apport alimentaire et hydrique, l'activité et l'examen général) ou à la nécropsie. Les tumeurs traitées présentent des niveaux diminués d'Akt et de S6 phosphorylés, ce qui est cohérent avec le blocage de p110α et de mTOR. Ce traitement est cytostatique pour les xénogreffes de gliome.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/16647110/ [2] https://pubmed.ncbi.nlm.nih.gov/16697955/ [3] https://pubmed.ncbi.nlm.nih.gov/19584227/

Applications (Applications)

Méthodes	Biomarqueurs	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

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):