PI3K inhibitor,selective, reversible and ATP-competitive
CAS：1173204-81-3
分子式：C29H34N10O3
分子量：570.65
纯度：98%
存储：Store at -20°C

Background:

PKI-402 is a selective, equipotent and ATP-competitive class I PI3K inhibitor (IC50= 1 nM, 7 nM, 16 nM and 14 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively.)

 

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.

 

In multiple human cancer cell lines (e.g. breast, brain, pancreas and NSCL), PKI-402 inhibited growth of cancer cells, and attenuated phosphorylation of effector of PI3K and mTOR. In MDA-MB-361, 30 nM PKI-402 caused cleaved of the apoptosis marker—PARP.

 

In MDA-MB-361 mouse tumor xenograft models, administration of 100 mg/kg of PKI-402 daily for 5 days decreased the initial tumor volume from 260 mm³to 129 mm³and inhibited tumor regrowth for 70 days, single dose of PKI-402 blocked phosphorylation of Akt and led to cleaved PARP.

 

 

Reference:

 1. Mallon R, Hollander I, Feldberg L et al. Antitumor efficacy profile of PKI-402, a dual phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor. Mol Cancer Ther. 2010 Apr;9(4):976-84.