400-920-2911 sales@csnpharm.cn
您的位置 : 首页 / PI3K/Akt/mTOR / PI3K & Autophagy & ATM/ATR / PI-103
CAS No.: 371935-74-9
Synonyms: PI-103
PI-103 is a potent inhibitor with low IC50 values against recombinant PI3K isoforms p110alpha (IC50= 2 nM), p110beta (IC50= 3 nM), p110delta (IC50= 3 nM), and p110gamma (IC50= 15 nM), less potent to mTOR/DNA-PK with IC50 of 30 nM/23 nM. It blocks autophagic flux.
生物活性
靶点 | DNA-PK IC50:23nM | mTOR IC50:30nM | p110α IC50:2nM | p110β IC50:3nM | p110γ IC50:15nM | 更多 |
实验方案
技术信息
CAS号 | 371935-74-9 | 储存条件 |
|
|||||||||||||
分子式 | C19H16N4O3 | 运输 | 蓝冰 | |||||||||||||
分子量 | 348.36 | 别名 | PI-103 | |||||||||||||
溶解度 |
|
动物实验配方 |
|
Cell Lines | Concentration | Assay Type | Time | Activity Description | Data Sources |
---|
518A2 | 0.01–10 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 21048785 |
518A2 | 0.001–1 μM | Function Assay | 24 h | suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets | 21048785 |
A549 | 0.25/0.5/1 μM | Function Assay | 24 h | inhibits Akt phosphorylation slightly | 24351425 |
A549 | 0-3.3 μM | Function Assay | 72 h | induces complete downregulation of pAKT | 23259591 |
AGS HG | - | Growth Inhibition Assay | - | IC50=0.68 ± 0.031 μM | 24597478 |
AGS LG | - | Growth Inhibition Assay | - | IC50=0.05 ± 0.001 μM | 24597478 |
ALL-SIL | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
BT549 | 0-3 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 25721419 |
CCRF-CEM | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
DETROIT562 | - | Growth Inhibition Assay | - | IC50=0.13 μM | 19584227 |
DND41 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
FaDu | 0.25/0.5/1 μM | Function Assay | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
G 35 DC | 0.05-20 μM | Growth Inhibition Assay | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
G 35 SC | 0.05-20 μM | Growth Inhibition Assay | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
G 38 DC | 0.05-20 μM | Growth Inhibition Assay | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
G 38 SC | 0.05-20 μM | Growth Inhibition Assay | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
G 40 DC | 0.05-20 μM | Growth Inhibition Assay | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
G 40 SC | 0.05-20 μM | Growth Inhibition Assay | 24/72 h | inhibits cell viability dose and time dependently | 26121251 |
H3122 | 0-3.3 μM | Function Assay | 72 h | induces complete downregulation of pAKT | 23259591 |
H460 | 0.25/0.5/1 μM | Function Assay | 24 h | inhibits Akt phosphorylation slightly | 24351425 |
H661 | 0.25/0.5/1 μM | Function Assay | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
HCC1937 | 1 μM | Function Assay | 24 h | reduces the phosphorylation of AKT | 22488590 |
HCC827 | 0-3.3 μM | Function Assay | 72 h | induces complete downregulation of pAKT | 23259591 |
HCC827 | 0-3 μM | Growth Inhibition Assay | 72 h | IC50=0.3 μM | 21220474 |
HGC27 HG | - | Growth Inhibition Assay | - | IC50=0.38 ± 0.022 μM | 24597478 |
HGC27 LG | - | Growth Inhibition Assay | - | IC50=0.02 ± 0.004 μM | 24597478 |
HPB-ALL | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
HS578T | 0-3 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 25721419 |
HS578T | 0.01-10 μM | Function Assay | 24 h | downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins | 25721419 |
HT1080 | 3 µM | Apoptosis Assay | 12 h | sensitizes RD cells to DOX-induced apoptosis | 23300809 |
HUVEC | - | Growth Inhibition Assay | - | IC50=0.08 μM | 19584227 |
IGROV-1 | - | Growth Inhibition Assay | - | IC50=0.06 μM | 19584227 |
Jurkat | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
Karpas-45 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
KE37 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
KMS12-BM | 0-2 μM | Growth Inhibition Assay | 24 h | IC50>2 μM | 22829234 |
LN229 | 1 μM | Function Assay | 48 h | induces autophagosome formation | 21062993 |
LOUCY | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
MDA-MB-231 | 0-3 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 25721419 |
MDA-MB-231 | 0.01-10 μM | Function Assay | 24 h | downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins | 25721419 |
MDA-MB-231 | 0.3 μM | Cell Viability Assay | 72 h | enhances cytotoxic effects of PI3K/AKT pathway inhibitors | 23601074 |
MDA-MB-436 | 0-3 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 25721419 |
MDA-MB-436 | 1 μM | Function Assay | 24 h | reduces the phosphorylation of AKT | 22488590 |
MDA-MB-468 | 0-3 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 25721419 |
MDA-MB-468 | 0.01-10 μM | Function Assay | 24 h | downregulates the levels of β-TrCP1, c-Myc and cyclin E proteins | 25721419 |
MDA-MB-468 | 0.3 μM | Cell Viability Assay | 72 h | enhances cytotoxic effects of PI3K/AKT pathway inhibitors | 23601074 |
Mel-Juso | 0.01–10 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 21048785 |
Mel-Juso | 0.001–1 μM | Function Assay | 24 h | suppresses phosphorylation of phosphatidyl inositol 3-kinase downstream targets | 21048785 |
MKN45 HG | - | Growth Inhibition Assay | - | IC50=1.01 ± 0.051 μM | 24597478 |
MKN45 LG | - | Growth Inhibition Assay | - | IC50=0.87 ± 0.030 μM | 24597478 |
MM1S | 0-2 μM | Growth Inhibition Assay | 24 h | IC50=0.5 μM | 22829234 |
MOLT-16 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
MOLT-4 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
NCI-H929 | 0-2 μM | Growth Inhibition Assay | 24 h | IC50=0.25 μM | 22829234 |
NUGC4 HG | - | Growth Inhibition Assay | - | IC50=14.0 ± 3.913 μM | 24597478 |
NUGC4 LG | - | Growth Inhibition Assay | - | IC50=14.0 ± 5.321 μM | 24597478 |
PC3 | - | Growth Inhibition Assay | 24h | GI50 = 100 nM | 20551061 |
PC3 | - | Growth Inhibition Assay | - | IC50=0.10 μM | 19584227 |
PC-9 | 0-3 μM | Growth Inhibition Assay | 72 h | IC50=0.8 μM | 21220474 |
PEER | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
PF-382 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
RD | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces apoptosis combined with GANT61 | 25749378 |
RD | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
RD | 3 µM | Apoptosis Assay | 12 h | sensitizes RD cells to DOX-induced apoptosis | 23300809 |
RH30 | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces apoptosis combined with GANT61 | 25749378 |
RH30 | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
RMS13 | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces apoptosis combined with GANT61 | 25749378 |
RMS13 | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
RPMI-8402 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
SAS | 0.25/0.5/1 μM | Function Assay | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
SF767 | 1 μM | Function Assay | 48 h | induces autophagosome formation | 21062993 |
SH-SY5Y | 0-8 μM | Growth Inhibition Assay | 24/48/72 h | induces time- and concentration-dependent inhibition on NB cell growth | 26224681 |
SH-SY5Y | 1 μM | Apoptosis Assay | 0.5-24 h | sensitizes neuroblastoma cells to doxorubicin-induced apoptosis | 26224681 |
SK-N-BE | 0-8 μM | Growth Inhibition Assay | 24/48/72 h | induces time- and concentration-dependent inhibition on NB cell growth | 26224681 |
SKNBE(2c) | 1.5/2.5/5 μM | Function Assay | 24 h | induces G1 cell-cycle arrest and apoptosis | 23378341 |
SKOV-3 | - | Growth Inhibition Assay | - | IC50=0.12 μM | 19584227 |
SUM1315MO2 | 1 μM | Function Assay | 24 h | reduces the phosphorylation of AKT | 22488590 |
SUM149PT | 0-3 μM | Cell Viability Assay | 72 h | inhibits cell viability dose dependently | 25721419 |
SUM149PT | 0.3 μM | Cell Viability Assay | 72 h | enhances cytotoxic effects of PI3K/AKT pathway inhibitors | 23601074 |
SUM149PT | 1 μM | Function Assay | 24 h | reduces the phosphorylation of AKT | 22488590 |
SUP-T1 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
SW872 | 0.01-0.5 μM | Function Assay | 24 h | reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner | 24695632 |
SW872 | 0.01-0.5 μM | Apoptosis Assay | 48 h | induces apoptosis dose dependently | 24695632 |
SW982 | 0.01-0.5 μM | Function Assay | 24 h | reduces AKT phosphorylation (pAKT) and 4EBP1 phosphorylation (p4EBP1) in a dose-dependent manner | 24695632 |
SW982 | 0.01-0.5 μM | Apoptosis Assay | 48 h | induces apoptosis dose dependently | 24695632 |
SY5Y | 1.5/2.5/5 μM | Function Assay | 24 h | induces G1 cell-cycle arrest and apoptosis | 23378341 |
TALL-1 | 1 μM | Growth Inhibition Assay | 7 d | decreases the cell number significantly | 23038273 |
TE381.T | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces apoptosis combined with GANT61 | 25749378 |
TE671 | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces caspase-dependent apoptosis combined with UO126 | 23684925 |
TP5014 | 3 µM | Apoptosis Assay | 12 h | sensitizes RD cells to DOX-induced apoptosis | 23300809 |
U118MG | 0.1-1 μM | Function Assay | 24 h | inhibits PI3K-mediated signaling | 19633683 |
U138MG | 0.1-1 μM | Function Assay | 24 h | inhibits PI3K-mediated signaling | 19633683 |
U373 | 1 μM | Function Assay | 48 h | induces autophagosome formation | 21062993 |
U87 | 1 μM | Function Assay | 48 h | induces autophagosome formation | 21062993 |
U87MG | 0.1-1 μM | Function Assay | 24 h | inhibits PI3K-mediated signaling | 19633683 |
U87MG | - | Growth Inhibition Assay | - | IC50=0.14 μM | 19584227 |
UCH-1 | 0-5 μM | Function Assay | - | inhibits the phosphorylation of both AKT and mTOR in a dose-dependent manner | 19528441 |
UCH-1 | 0.01-10 μM | Growth Inhibition Assay | 6 d | inhibits proliferation dose dependently | 19528441 |
UCH-1 | 0.1-10 μM | Apoptosis Assay | 24 h | induces apoptosis | 19528441 |
UT5 | 0.25/0.5/1 μM | Function Assay | 24 h | inhibits Akt phosphorylation significantly | 24351425 |
VJ | 1/1.5/2 μM | Apoptosis Assay | 72 h | induces apoptosis combined with GANT61 | 25749378 |
靶点 | Description | IC50 |
---|---|---|
DNA-PK | IC50:23nM | |
mTOR | IC50:30nM | |
p110α | IC50:2nM | |
p110β | IC50:3nM | |
p110γ | IC50:15nM | |
p110δ | IC50:3nM |
联系我们
官方电话:400-920-2911
二维码
微信公众号 CSN官网