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CAS No. : 1197160-28-3
MCE 国际站:PKI-179
产品活性:PKI-179 是一种有效的和具有口服活性的双重 PI3K/mTOR 抑制剂,对 PI3K-α,PI3K-β,PI3K-γ,PI3K-δ 和 mTOR 的 IC50 值分别为 8 nM,24 nM,74 nM,77 nM 和 0.42 nM。PKI-179 还表现出对 E545K 和 H1047R 的活性,IC50 值分别为 14 nM 和 11 nM。PKI-179 在体内显示出抗肿瘤活性。
研究领域:PI3K/Akt/mTOR
作用靶点:PI3K | mTOR
In Vitro: PKI-179 inhibits the cell proliferation, with IC50s of 22 nM and 29 nM for MDA361 and PC3 cells, respectively.
PKI-179 shows inhibitory activity against a panel of 361 other kinases, hERG and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM, but does have activity for CYP2C8 (IC50=3 μM).
In Vivo: PKI-179 (5-50 mg/kg; p.o. once daily for 40 days) inhibits the tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors.
PKI-179 (50 mg/kg; p.o.) results in good inhibition of PI3K signaling in nude mice bearing MDA361 tumor xenografts.
PKI-179 exhibits good oral bioavailability (98% in nude mouse, 46% in rat, 38% in monkey, and 61% in dog) and a high half-life (>60 min) .
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