产品描述:
CH5132799 is an inhibitor of class I PI3K isoforms (IC50s = 14, 120, 500, and 36 nM for PI3Kα, PI3Kβ, PI3Kδ, and PI3Kγ, respectively).{42659} It is selective for these PI3K isoforms over PI3KC2α and PI3KC2β, which are class II PI3Ks, Vps34, a class III PI3K, and mTOR (IC50s = 5,300, >10,000, >10,000, and 1,600 nM, respectively), as well as 26 additional protein kinases (IC50s = >10,000 nM). CH5132799 inhibits proliferation of HCT116, KPL-4, T47D, and SKOV3 cancer cells expressing the activating mutation PI3KαH1047R (IC50s = 200, 32, 56, and 120 nM, respectively). It also reduces tumor growth in a PC3 mouse xenograft model when administered at a dose of 25 mg/kg per day.