产品描述:
Inavolisib is an inhibitor of PI3Kα (Ki = 0.034 nM).{51583} It is selective for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ (Kis = 99.7, 12.2, and 18.2 nM, respectively) and is 4.4-fold selective in decreasing the phosphorylated levels of proline-rich Akt substrate 40 kDa (PRAS40) in HCC1954 breast cancer cells, which express wild-type PI3K catalytic subunit p110α and p110α containing a histidine-to-arginine mutation at position 1047 (p110αH1047R), over HDQ-P1 breast ductal carcinoma cells, which express only wild-type p110α. Inavolisib (111 nM) induces poly(ADP-ribose) polymerase (PARP) cleavage, a marker of apoptosis, in HCC1954 cells. It reduces the levels of phosphorylated Akt, PRAS40, and mutant p110α in HCC1954 cells, but not HDQ-P1 cells, when used at concentrations of 111, 333, and 1,000 nM. In vivo, inavolisib (25 or 50 mg/kg per day) decreases tumor volume in an HCC1954 mouse xenograft model.