S63845 是一种有效的选择性骨髓细胞白血病 1 (MCL1) 抑制剂，结合人 MCL1 的 K_d 值为 0.19 nM。

S63845 is a potent and selective myeloid cell leukemia 1 (MCL1) inhibitor with a K d of 0.19 nM for human MCL1.

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MCL1 0.19 nM (Kd)

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). has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[1]. Kotschy A, et al. The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models. Nature. 2016 Oct 27;538(7626):477-482.

In Vitro: DMSO : 33.33 mg/mL (40.19 mM; Need ultrasonic)配制储备液