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PI-103

PI-103 是一種多靶點 PI3K 抑制劑，在無細胞試驗中作用于p110α/β/δ/γ的IC50為 2 nM/3 nM/3 nM/15 nM，對 mTOR/DNA-PK的作用較小，IC50為30 nM/23 nM。PI-103 可誘導(dǎo)小鼠T細胞淋巴瘤的凋亡。

PI-103 Chemical Structure

PI-103 Chemical Structure

CAS: 371935-74-9

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1103.62 現(xiàn)貨
5mg 1211.49 現(xiàn)貨
25mg 3023.41 現(xiàn)貨
50mg 4832.1 現(xiàn)貨
100mg 6470.64 現(xiàn)貨
200mg 11220.3 現(xiàn)貨
1g 27764.34 現(xiàn)貨
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PI-103相關(guān)產(chǎn)品

相關(guān)信號通路圖

PI3K Signaling Pathways

PI3K信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 PI-103 是一種多靶點 PI3K 抑制劑，在無細胞試驗中作用于p110α/β/δ/γ的IC50為 2 nM/3 nM/3 nM/15 nM，對 mTOR/DNA-PK的作用較小，IC50為30 nM/23 nM。PI-103 可誘導(dǎo)小鼠T細胞淋巴瘤的凋亡。
特性 PI-103是第一個有效合成的mTOR抑制劑。
靶點
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)		 點擊更多
2 nM 3 nM 3 nM 15 nM 23 nM
體外研究(In Vitro)
體外研究活性

PI-103有效抑制蛋白激酶mTOR的對apamycin敏感的(mTORC1)和對rapamycin不敏感的(mTORC2)復(fù)合物。PI-103是第三大多靶點PI3K抑制劑。[1]PI-103抑制組成型和生長因子誘導(dǎo)的PI3K/Akt和mTORC1激活。在胚細胞中，尤其在白血病干細胞中，PI-103抑制白血病細胞增殖和白血病前體細胞形成集落，且誘導(dǎo)線粒體細胞凋亡。PI-103抑制p110α的效果比抑制p110β強200倍以上。PI-103也有效抑制脂肪細胞中的PI(3,4)P2和PIP3，及肌管中的PIP3。與LY294002抑制Akt磷酸化的IC50值相比，PI-103抑制Akt磷酸化的IC50值要低到100倍。PI-103保護動物使其免受胰島素刺激而導(dǎo)致的血糖降低。PI-103聯(lián)用作用于胚細胞和不成熟的白血病細胞有增強凋亡的功效。[2]
激酶實驗 p110激酶實驗
加入含10 μCi γ-32P-ATP 的ATP開始反應(yīng)，終濃度為10 或100 μM,在室溫下進行20分鐘。用于分析 TLC,加入105 μL 1 N HCl，然后加入160μL CHCl3:MeOH (1:1)，反應(yīng)終止。渦旋兩相混合物,簡單離心，使用CHCl3預(yù)包被的凝膠上樣吸頭將有機相轉(zhuǎn)移到新的試管中。TLC板上染色提取物，然后在n-丙醇:1 M乙酸的溶液中進行3到4小時。然后烘干TLC板, 然后用感光成像系統(tǒng)處理，再進行量化。測定PI-103,用10-12種濃度從實驗所用最高濃度(100 μM)稀釋2倍的抑制劑進行激酶活性測定。測定IC50重復(fù)進行2到4次，取幾次獨立測量的平均值。
細胞實驗 細胞系 U87MG細胞
濃度 0.5 μM
孵育時間 24小時
方法

評估細胞死亡，用PI-103處理U87MG細胞24小時。通過LDH活性的比色測定，用細胞毒性檢測試劑盒測量細胞死亡。按公式:[(實驗值-低對照值)/(高對照值-低對照值)×100]計算死亡百分率（3個12孔板每個實驗點的平均值)，低對照細胞用DMSO處理的，高對照細胞用1% Triton X-100在37oC下處理30分鐘。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

當(dāng)腫瘤達到50-100 mm3時, 動物隨機分組，用PI-103處理，及空白對照處理。PI-103具有明顯活性,處理18天后，使腫瘤平均尺寸降低4倍。用PI-103處理的鼠在發(fā)病前或驗尸時沒有明顯毒性現(xiàn)象(根據(jù)體重，食物和水?dāng)z取情況，活動性, 及常規(guī)檢查)。處理的腫瘤Akt和S6磷酸化水平明顯降低,伴隨著p110α和mTOR被抑制。PI-103處理神經(jīng)膠質(zhì)移植瘤，抑制生長。[2]
動物實驗 Animal Models 左前肢末端皮下注射U87MG:106個ΔEGFR 細胞的6到12周大Balbc nu/nu鼠
Dosages 5 mg/kg
Administration 腹腔注射

化學(xué)信息&溶解度

分子量 348.36 分子式

C19H16N4O3
CAS號 371935-74-9 SDF Download PI-103 SDF
Smiles C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 24 mg/mL ( (68.89 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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