CH5132799 ( CH5132799; CH-5132799; PA799; PA-799. )

产品货号. M17113 CAS No. 1007207-67-1

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产品名称

CH5132799
注意事项

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断
产品简述

CH5132799 has been used in trials studying the treatment of Solid Tumors.
产品描述

CH5132799, also known as PA-799, is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice. CH5132799 selectively inhibited class I PI3Ks and PI3Kα mutants in in vitro kinase assays. Tumors harboring PIK3CA mutations were significantly sensitive to CH5132799 in vitro and were remarkably regressed by CH5132799 in in vivo mouse xenograft models.
同义词

CH5132799; CH-5132799; PA799; PA-799.
通路

Others
靶点

Other Targets
受体

mTOR; PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
研究领域

Cancer
适应症

——

CAS Number

1007207-67-1
分子量

377.42
分子式

C15H19N7O3S
纯度

98%
溶解度

DMSO : 4.55 mg/mL 12.06 mM;H2O : < 0.1 mg/mL
SMILES

CS(=O)(=O)N1CCc2c(nc(nc12)N1CCOCC1)c1cnc(N)nc1
化学全称

5-(7-(methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine

1. Tanaka H, et al, Clin Y Res, 2011, 17(10), 3272-3281.

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