PI-103

製品コード：S1038 純度：99.59%

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.

CAS No. 371935-74-9

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
10mg	JPY 40500	国内在庫あり
25mg	JPY 55500	国内在庫あり
1g	JPY 448500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（99）

製品安全説明書

現在のバッチを見る：純度： 99.59%

99.59

PI-103関連製品

関連ターゲット	p110α p110β p110δ p110γ C2β Vps34	もっと見る
関連製品	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 AZD6482 Gedatolisib (PKI-587) HS-173 AS-252424 Eganelisib (IPI-549) VS-5584 (SB2343) GSK2636771 AZD8186 GSK1059615 Pilaralisib (XL147) TG100-115 CZC24832 Voxtalisib (XL765) XL147 analogue AS-604850 BGT226 (NVP-BGT226) maleate Quercetin Dihydrate VPS34 inhibitor 1 (Compound 19) Samotolisib (LY3023414) Voxtalisib (XL765) Analogue AMG319 Nemiralisib Bimiralisib (PQR309) CH5132799 PKI-402 TG100713 Paxalisib (GDC-0084) SF2523 Serabelisib (TAK-117) GDC-0326 GNE-317 Inavolisib (GDC-0077) PIK-294 PI-3065 AZD8835 Seletalisib (UCB-5857) leniolisib (CDZ 173) (E)-Akt inhibitor-IV Gallein CAY10505 Selective PI3Kδ Inhibitor 1 (compound 7n) PF-4989216 GNE-477 GNE-493	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library Apoptosis Compound Library Cell Cycle compound library NF-κB Signaling Compound Library	もっと見る

シグナル伝達経路

PI3Kシグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
RH30	Apoptosis Assay	1/1.5/2 μM	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RMS13	Apoptosis Assay	1/1.5/2 μM	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
SUM149PT	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
MDA-MB-231	Cell Viability Assay	0.3 μM	72 h	enhances cytotoxic effects of PI3K/AKT pathway inhibitors	23601074
SY5Y	Function Assay	1.5/2.5/5 μM	24 h	induces G1 cell-cycle arrest and apoptosis	23378341
SKNBE(2c)	Function Assay	1.5/2.5/5 μM	24 h	induces G1 cell-cycle arrest and apoptosis	23378341
RD	Apoptosis Assay	3 µM	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
TP5014	Apoptosis Assay	3 µM	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
HT1080	Apoptosis Assay	3 µM	12 h	sensitizes RD cells to DOX-induced apoptosis	23300809
A549	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
H3122	Function Assay	0-3.3 μM	72 h	induces complete downregulation of pAKT	23259591
TALL-1	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
DND41	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
PEER	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
KE37	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
RPMI-8402	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
MOLT-4	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
CCRF-CEM	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
MOLT-16	Growth Inhibition Assay	1 μM	7 d	decreases the cell number significantly	23038273
MM1S	Growth Inhibition Assay	0-2 μM	24 h	IC50=0.5 μM	22829234
NCI-H929	Growth Inhibition Assay	0-2 μM	24 h	IC50=0.25 μM	22829234
KMS12-BM	Growth Inhibition Assay	0-2 μM	24 h	IC50＞2 μM	22829234
MDA-MB-436	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
SUM1315MO2	Function Assay	1 μM	24 h	reduces the phosphorylation of AKT	22488590
HCC1937	Function Assay	1 μM	24 h	reduces the phosphorylation of AKT	22488590
HCC827	Growth Inhibition Assay	0-3 μM	72 h	IC50=0.3 μM	21220474
PC-9	Growth Inhibition Assay	0-3 μM	72 h	IC50=0.8 μM	21220474
LN229	Function Assay	1 μM	48 h	induces autophagosome formation	21062993
U87	Function Assay	1 μM	48 h	induces autophagosome formation	21062993
U373	Function Assay	1 μM	48 h	induces autophagosome formation	21062993
SF767	Function Assay	1 μM	48 h	induces autophagosome formation	21062993
Mel-Juso	Cell Viability Assay	0.01–10 μM	72 h	inhibits cell viability dose dependently	21048785
518A2	Cell Viability Assay	0.01–10 μM	72 h	inhibits cell viability dose dependently	21048785
Mel-Juso	Function Assay	0.001–1 μM	24 h	suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
518A2	Function Assay	0.001–1 μM	24 h	suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets	21048785
U87MG	Function Assay	0.1-1 μM	24 h	inhibits PI3K-mediated signaling	19633683
U138MG	Function Assay	0.1-1 μM	24 h	inhibits PI3K-mediated signaling	19633683
U118MG	Function Assay	0.1-1 μM	24 h	inhibits PI3K-mediated signaling	19633683
UCH-1	Growth Inhibition Assay	0.01-10 μM	6 d	inhibits proliferation dose dependently	19528441
UCH-1	Apoptosis Assay	0.1-10 μM	24 h	induces apoptosis	19528441
TE671	Apoptosis Assay	1/1.5/2 μM	72 h	induces caspase-dependent apoptosis combined with UO126	23684925
RD	Apoptosis Assay	1/1.5/2 μM	72 h	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
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	inhibits cell viability dose and time dependently	26121251
G 38 DC	Growth Inhibition Assay	0.05-20 μM	24/72 h	inhibits cell viability dose and time dependently	26121251
G 35 DC	Growth Inhibition Assay	0.05-20 μM	24/72 h	inhibits cell viability dose and time dependently	26121251
G 40 SC	Growth Inhibition Assay	0.05-20 μM	24/72 h	inhibits cell viability dose and time dependently	26121251
G 38 SC	Growth Inhibition Assay	0.05-20 μM	24/72 h	inhibits cell viability dose and time dependently	26121251
G 35 SC	Growth Inhibition Assay	0.05-20 μM	24/72 h	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
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
UCH-1	Function Assay	0-5 μM		inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner	19528441
HEK293	Function assay	0.5uM		Inhibition of PKB-S473 phosphorylation in IGF-1 treated HEK293 cells at 0.5uM	17850214
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
PC3	Growth Inhibition Assay		24h	GI50 = 100 nM	20551061
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
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
U87MG	Growth Inhibition Assay			IC50=0.14 μM	19584227
IGROV-1	Growth Inhibition Assay			IC50=0.06 μM	19584227
DETROIT562	Growth Inhibition Assay			IC50=0.13 μM	19584227
PC3	Growth Inhibition Assay			IC50=0.10 μM	19584227
SKOV-3	Growth Inhibition Assay			IC50=0.12 μM	19584227
HUVEC	Growth Inhibition Assay			IC50=0.08 μM	19584227
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
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
MCF7	Antiproliferative assay			Antiproliferative activity against human MCF7 cells, IC50=22.4μM.	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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

特性

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)	もっとクリックする
2 nM	3 nM	3 nM	15 nM	23 nM	もっとクリックする

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.
細胞実験	細胞株	U87MG cells
	濃度	0.5 μM
	反応時間	24 hours
	実験の流れ	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 °
実験結果図	Methods	Biomarkers	結果図	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]
動物実験	動物モデル	6- to 12-week-old Balbc nu/nu mice bearing U87MG:ΔEGFR cells
	投与量	5 mg/kg
	投与経路	Administered via i.p.

参考
[1] Knight ZA, et al. Cell, 2006, 125(4), 733-747. [2] Fan QW, et al. Cancer Cell, 2006, 9(5), 341-349. [3] Raynaud FI, et al. Mol Cancer Ther. 2009, 8(7), 1725-1738.

参考

化学情報

分子量	348.36	化学式	C₁₉H₁₆N₄O₃
CAS No.	371935-74-9	SDF	Download PI-103 SDFをダウンロードする
Smiles	C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 24 mg/mL ( (68.89 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

* 大学・企業名 大学・企業名を記入してください

* 名前 名前を記入してください

* 電子メール 電子メール・アドレスを記入してください 有効なメールアドレスを入力してください

電話番号

* 内容 お問い合わせ内容をご入力ください

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):