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S63845

CAS No. : 1799633-27-4

MCE 國(guó)際站：S63845

產(chǎn)品活性：S63845 是一種有效的選擇性骨髓細(xì)胞白血病 1 (MCL1) 抑制劑，結(jié)合人 MCL1 的 K_d 值為 0.19 nM。

研究領(lǐng)域：Apoptosis

作用靶點(diǎn)：Bcl-2 Family

In Vitro: The pro-survival protein myeloid cell leukemia 1 (MCL1) is over expressed in many cancers. S63845 is a small molecule that specifically binds with high affinity to the BH3-binding groove of MCL1. S63845 potently kills MCL1-dependent cancer cells, including multiple myeloma, leukaemia and lymphoma cells, by activating the BAX/BAK-dependent mitochondrial apoptotic pathway. The activity of S63845 is next evaluated in a panel of eight AML cell lines: all lines are sensitive to S63845 (IC₅₀=4-233 nM).

In Vivo: S63845 shows potent anti-tumour activity with an acceptable safety margin as a single agent in several cancers. Intravenously injected (i.v.) S63845 exerts dose-dependent anti-tumour activity in human multiple myeloma (H929 and AMO1) xenografts in immunocompromised mice, with maximal tumour growth inhibition of 114% in the AMO1 model and 103% in the H929 model. At 25 mg/kg, S63845 induces complete regression in 7 out of 8 of the mice at 100 days after treatment in the AMO1 model.

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