AGI-6780

AGI-6780CAS号: 1432660-47-3分子式: C21H18F3N3O3S2分子量: 481.5描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)

产品描述
描述
AGI-6780 is the first highly potent and selective small molecule inhibitor of isocitrate dehydrogenases, which binds in an allosteric manner at the dimer interface of mutant IDH2-R140Q (IC50=23 nM).
纯度
>98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
AGI 6780; AGI6780
外观
Powder
可溶性/溶解性
DMSO 96 mg/mL (199.37 mM)

Ethanol 96 mg/mL (199.37 mM)

生物活性
靶点
IDH2 R140Q mutant
In vitro(体外研究)
AGI-6780 potently reduce (R)-2-hydroxyglutarate (2HG) levels in cell lines ectopically overexpressing IDH2/R140Q with EC50 of 20 nM, with excellent selectivity against other dehydrogenases. AGI-6780 reverses the IDH2/R140Q-induced differentiation block in TF-1 cells, and induces blast differentiation in primary human IDH2/R140Q AML patient samples.

分子结构图

AGI-6780