Murizatoclax(Synonyms: AMG 397)

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Murizatoclax (Synonyms: AMG 397)

Murizatoclax (AMG 397) 是一种有效，选择性和具有口服活性的髓样白血病 1 (MCL-1) 抑制剂，Ki 值为 15 pM。Murizatoclax 与促凋亡 BCL-2 家族成员竞争性结合 MCL1 的 BH3 结合沟。Murizatoclax 可用于癌症的研究。

Murizatoclax(Synonyms: AMG 397)

Murizatoclax Chemical Structure

CAS No. : 2245848-05-7

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生物活性

Murizatoclax (AMG 397) is a potent, selective and orally active inhibitor of myeloid leukemia 1 (MCL-1) inhibitor, with a Ki of 15 pM. Murizatoclax competitive binds to the BH3-binding groove of MCL1 with pro-apoptotic BCL-2 family members. Murizatoclax can be used for the research of cancer[1][2].

IC50 & Target[1]

MCL1

15 pM (Ki)

体外研究
(In Vitro)

AMG 397 potently disrupts the interaction between MCL1 and BIM in OPM2 cells, induces clear increases in Caspase-3/7 activity within one hour[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Murizatoclax (25-50 mg/kg; p.o. once or twice weekly) exhibits significant tumor regressions in mice bearing OPM2 xenografts[2].
Murizatoclax (10-60 mg/kg; p.o. twice weekly) achieves 47% MOLM-13 orthotopic tumor growth inhibition (TGI), 99% TGI and 75% regression at the dose of 10, 30 and 60 mg/kg, respectively[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

765.44

Formula

C42H57ClN4O5S
CAS 号

2245848-05-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Wang H, et, al. Targeting MCL-1 in cancer: current status and perspectives. J Hematol Oncol. 2021 Apr 21;14(1):67.

    [2]. Caenepeel S, et al. Abstract 6218: discovery and preclinical evaluation of AMG 397, a potent, selective and orally bioavailable MCL1 inhibitor. Cancer Res. 2020;80(16 Supplement):6218.

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