生物活性 | |||
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描述 | BAY-1436032, identified as a comprehensive mutant IDH1 inhibitor, curtails the production of intracellular (R)-2-hydroxyglutarate (R-2HG) in mouse hematopoietic cells harboring IDH1R132H or IDH1R132C mutations, with IC50s of 60 and 45 nM, respectively. It does not affect R-2HG levels in cells expressing IDH2R140Q and IDH2R172K up to a concentration of 10 μM. A 0.1 μM concentration of BAY-1436032 inhibits colony growth by 50%, while up to 100 μM does not hinder the colony growth of AML cells with wild-type IDH1. BAY-1436032 notably induces myelomonocytic differentiation in myeloid progenitors[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.21mL 2.04mL 1.02mL |
20.43mL 4.09mL 2.04mL |
参考文献 |
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