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Ipatasertib dihydrochloride

CAS No. : 1396257-94-5

MCE 站：Ipatasertib dihydrochloride

产品活性：Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) 是一种选择性的，ATP竞争性的 pan-Akt 抑制剂，抑制 Akt1，Akt2，Akt3 的 IC₅₀ 分别为 5，18，8 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：Akt

In Vitro: Ipatasertib shows more than 600 ａnd more than 100-fold selectivity for Akt1 in IC₅₀ against the closely related kinases PKA ａnd p70S6K, respectively. When tested at 1 μM in a panel of 230 protein kinases, which includes 36 human AGC family members, Ipatasertib inhibits only 3 other kinases by more than 70% at 1 μM concentration (PRKG1α, PRKG1β, ａnd p70S6K). IC₅₀s measured for these 3 kinases are 98, 69, ａnd 860 nM, respectively. Thus, with the exception of PKG1 (relative to which Ipatasertib is >10-fold more selective for Akt1), Ipatasertib displays a more than 100-fold selectivity for Akt1 over the next most potently inhibited non-Akt kinase, p70S6K, in the screening kinase panel. The relationship between pharmacokinetics (PK) ａnd pharmacodynamics (PD) of Ipatasertib is investigated in 3 xenograft models that showed dose-dependent response to drug treatment: MCF7-neo/HER2, TOV-21G.x1, ａnd LNCaP. The mean cell viability IC₅₀ of Ipatasertib in these 3 cell lines is 2.56, 0.44, ａnd 0.11 μM, respectively.

In Vivo: Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib in combination with RP-56976 induces tumor regression ａnd stasis in the PC-3 ａnd MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with NSC 241240. The combination of Ipatasertib with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone.

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