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BMS-536924

CAS No. : 468740-43-4

MCE 國(guó)際站：BMS-536924

產(chǎn)品活性：BMS-536924 是一種具有口服活性，競(jìng)爭(zhēng)性和選擇性的胰島素樣生長(zhǎng)因子受體 (IGF-1R) 激酶和胰島素受體 (IR) 抑制劑，IC₅₀ 分別為 100 nM 和 73 nM。BMS-536924 具有抗癌活性。

研究領(lǐng)域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶點(diǎn)：IGF-1R  |  Insulin Receptor  |  Apoptosis

In Vitro: BMS-536924 inhibits FAK and Lck with IC₅₀s of 150 nM and 341 nM, respectively.
BMS-536924 (1 μM; every four days for 12 days) blocks pBabe-MCF10A and CD8-IGF-IR-MCF10A acinar proliferation.
BMS-536924 (0.01-1 μM; 24 hours) inhibits growth of CD8-IGF-IR-MCF10A cells and has an IC₅₀ of 0.48 μM.
BMS-536924 (1 μM; for 4 days) induces apoptosis in CD8-IGF-IR-MCF10A acini.
BMS-536924 (0.1-1 μM; for 24 hours) decreases in S-phase cells and causes a G0/G1 block.
BMS-536924 (1 μM; 10 min, 1, 8, 24, 48 hours) inhibits IGF-IR signaling in pBabe-MCF10A cells and inhibits phosphorylation of CD8-IGF-IR. BMS-536924 time-dependently inhibits AKT phosphorylation.

In Vivo: BMS-536924 (100 mg/kg; gavage; daily; for 35 days) causes regression of xenografts in vivo and an average reduction of 76% tumor volume after 2 weeks.

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