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PI-103

PI3K inhibitor

Catalog No.S1038 Purity:99.59%

research use only

PI-103 is a multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. PI-103 induces apoptosis in murine T-cell Lymphoma.

PI-103 Chemical Structure

Molecular Weight: 348.36

Purity & Quality Control

Batch: Purity: 99.59%

99.59

PI-103 Related Products

Related Targets	p110α p110β p110δ p110γ C2β Vps34	Click to Expand
Related Products	LY294002 3-MA (3-Methyladenine) Dactolisib (BEZ235) Pictilisib (GDC-0941) Wortmannin Buparlisib (BKM120) TGX-221 ZSTK474 Omipalisib (GSK2126458) A66 PF-04691502 PIK-75 HCl IC-87114 740 Y-P (PDGFR 740Y-P) AS-605240 Taselisib (GDC 0032) SAR405 Apitolisib (GDC-0980) VPS34-IN1 PIK-90	Click to Expand
Related Compound Libraries	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	Click to Expand

Signaling Pathway

PI3K Signaling Pathway

Cell Culture and Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	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
Click to View More Cell Line Experimental Data

Mechanism of Action

Description

Features

The first potent, synthetic mTOR inhibitor.

Targets

p110α ^[3] (Cell-free assay)	p110β ^[3] (Cell-free assay)	p110δ ^[3] (Cell-free assay)	p110γ ^[3] (Cell-free assay)	DNA-PK ^[3] (Cell-free assay)	Click to View More Targets
2 nM	3 nM	3 nM	15 nM	23 nM	Click to View More Targets

In vitro
In vitro	PI-103 potently inhibits both the rapamycin-sensitive (mTORC1) and rapamycin-insensitive (mTORC2) complexes of the protein kinase mTOR. ^[1] PI-103 inhibits constitutive and growth factor-induced PI3K/Akt, as well as mTORC1 activation. ^[2] In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells. PI-103 inhibits p110α >200-fold more potently than p110β. PI-103 also potently blocks production of PI(3,4)P2 and PIP3 in adipocytes and PIP3 in myotubes. ^[2] PI-103 inhibits phosphorylation of Akt with an IC95 100-fold lower than that for LY294002. Strikingly, PI-103 completely protects animals from stimulated decline in blood glucose. PI-103 has additive proapoptotic effects in blast cells and in immature leukemic cells. ^[2]
Kinase Assay	Enzyme Assays
Kinase Assay	Phosphatidylinositide 3-kinase inhibitory activity was determined using a scintillation proximity assay in the presence of 1 μmol/L ATP. Inhibition of mTOR protein kinase was determined using a TR-FRET-based LanthaScreen method from Invitrogen. Compounds were assayed at a maximum concentration of 10 μmol/L in the presence of 1 μmol/L ATP, and IC50 values were determined using GraphPad Prism software.
Cell Research	Cell lines	U87MG cells
	Concentrations	0.5 μM
	Incubation Time	24 hours
	Method	U87MG cells are treated with PI-103 for 24 hours. Cell death is quantified by colorimetric determination of LDH activity using a cytotoxicity detection kit. Percentage of cell death (mean of three 12-well plates per experimental point) is calculated [(experimental value- low control)/(high control -low control) × 100], where the low-control cells are DMSO treated and high-control cells are Triton treated (1% Triton X-100, 30 min, 37 °
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	p-AKT / AKT / p-S6K / S6K / p-S6 / S6 / p-p38 / p38 p-GSK3 / GSK3 / p-BAD / BAD / p-MDM2 / MDM2 / p-p27 / p27 β-TrCP1 / p-mTOR		18922908
	Immunofluorescence	autophagosomes / autolysosomes		26814436
	Growth inhibition assay	Cell viability		25721419

In Vivo
In vivo	When tumors reach 50-100 mm³, animals are randomized and treated with vehicle or PI-103. PI-103 exhibits significant activity, decreasing average tumor size by 4-fold after 18 days. ^[2] Mice treated with PI-103 have no obvious signs of toxicity premorbidly (based on body weight, food and water intake, activity, and general exam) or at necropsy. Treated tumors display decreased levels of phosphorylated Akt and S6, consistent with blockade of p110α and mTOR. PI-103 treatment is cytostatic to glioma xenografts. ^[2]
Animal Research	Animal Models	6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
	Dosages	5 mg/kg
	Administration	Administered via i.p.

References
https://pubmed.ncbi.nlm.nih.gov/16647110/ https://pubmed.ncbi.nlm.nih.gov/16697955/ https://pubmed.ncbi.nlm.nih.gov/19584227/

References

https://pubmed.ncbi.nlm.nih.gov/16647110/
https://pubmed.ncbi.nlm.nih.gov/16697955/
https://pubmed.ncbi.nlm.nih.gov/19584227/

Chemical Information

Molecular Weight	348.36	Formula	C₁₉H₁₆N₄O₃
CAS No.	371935-74-9	SDF	Download PI-103 SDF
Synonyms	N/A
Smiles	C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O

Storage and Stability

Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
			1 month-20°Cin solvent

In vitro
Batch:

DMSO : 24 mg/mL ( (68.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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