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Serabelisib

CAS No. : 1268454-23-4

MCE 站：Serabelisib

产品活性：Serabelisib (MLN1117) 是一种选择性的 p110α 抑制剂, IC₅₀ 值为 15 nM。

研究领域：PI3K/Akt/mTOR

作用靶点：PI3K

In Vitro: Serabelisib (MLN1117) inhibits Akt phosphorylation and growth in PIK3CA mutant breast cancer cells with IC₅₀s around 2 μM, yet has no effect on cells lacking PTEN. BCR-stimulated B cells treated with 1 μM Serabelisib (MLN1117) displays a significant reduction (up to 50%) in the magnitude of the phosphorylated Akt (p-Akt) signal measured by intracellular flow cytometry. The effect of Serabelisib is dose-dependent.

In Vivo: Treatment with Serabelisib (MLN1117) at 30 and 60 mg/kg causes little reduction of TNP-specific IgG3. Notably, reduction of TNP-specific IgG3 at higher doses of Serabelisib (MLN1117) (120 mg/kg) is observed, consistent with the partial reduction in cell division in B cells treated with Serabelisib before anti-IgM stimulation. However, 120 mg/kg is above the effective dose of Serabelisib (MLN1117) for tumor growth inhibition (30-60 mg/kg).

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