Tapotoclax (AMG-176) 是一种有效的、有口服活性的、骨髓细胞因子 1 (MCL-1) 的选择性抑制剂,其 Ki 值为 0.13 nM。
产品详情
Tapotoclax (AMG-176) 是一种有效的、有口服活性的、骨髓细胞因子 1 (MCL-1) 的选择性抑制剂,其 Ki 值为 0.13 nM。
生物活性
Tapotoclax (AMG-176) is a potent, selective and orally active MCL-1 inhibitor, with a K i of 0.13 nM.
性状
Solid
IC50 & Target[1][2]
Mcl-1 0.13 nM (Ki)
体外研究(In Vitro)
Tapotoclax is an inhibitor of induced myeloid leukemia cell differentiation protein MCL-1 (Ki=0.13 nM), with potential pro-apoptotic and antineoplastic activities. Upon administration, Tapotoclax binds to and inhibits the activity of MCL-1. This disrupts the formation of MCL-1/Bcl-2-like protein 11 (BCL2L11; BIM) complexes and induces apoptosis in tumor cells. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Caenepeel S, et al. AMG 176, a Selective MCL1 Inhibitor, is Effective in Hematological Cancer Models Alone and in Combination with Established Therapies. Cancer Discov. 2018 Sep 25. pii: CD-18-0387.[2]. Garner TP, et al. Progress in targeting the BCL-2 family of proteins. Curr Opin Chem Biol. 2017 Aug;39:133-142.
溶解度数据
In Vitro: DMSO : 62.5 mg/mL (101.92 mM; Need ultrasonic)配制储备液
[1]. Caenepeel S, et al. AMG 176, a Selective MCL1 Inhibitor, is Effective in Hematological Cancer Models Alone and in Combination with Established Therapies. Cancer Discov. 2018 Sep 25. pii: CD-18-0387.[2]. Garner TP, et al. Progress in targeting the BCL-2 family of proteins. Curr Opin Chem Biol. 2017 Aug;39:133-142.