Uses
A selective, reversible and ATP-competitive Class I PI3K inhibitor. PI3Kα, IC50=1 nM; PI3Kβ, IC50=7 nM; PI3Kγ, IC50=16 nM; PI3Kδ, IC50=14 nM.
Biological Activity
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 mm3 to 129 mm3 and inhibited tumor regrowth for 70 days, single dose of pki-402 blocked phosphorylation of akt and led to cleaved parp.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.
