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PKI-179 hydrochloride

CAS No. : 1463510-35-1

MCE 站：PKI-179 hydrochloride

产品活性：PKI-179 hydrochloride 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 hydrochloride 还表现出对 E545K 和 H1047R 的活性，IC₅₀ 值分别为 14 nM 和 11 nM。PKI-179 hydrochloride 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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