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AGI5198
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产品介绍
产品介绍
产品信息
抗原名称
Isocitrate Dehydrogenase (IDH)
商品描述
AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.
分子量
462.56
纯度
>98%
可溶性
DMSO 24 mg/mL (51.88 mM)
Ethanol 14 mg/mL (30.26 mM)
Ethanol 14 mg/mL (30.26 mM)
外观
Powder
In vitro(体外研究)
Measurements of R-2HG concentrations in pellets of TS603 glioma cells demonstrates dose-dependent inhibition of the mutant IDH1 enzyme by AGI-5198. AGI-5198 does not impair colony formation of two patient-derived glioma lines that express only the wild-type IDH1 allele (TS676 and TS516). Cancer cells heterozygous for the IDH1(R132H) mutation exhibits less IDH-mediated production of NADPH, such that after exposure to ionizing radiation (IR), there are higher levels of reactive oxygen species, DNA double-strand breaks, and cell death compared with IDH1 wild-type cells. These effects are reversed by the IDH1(R132H) inhibitor AGI-5198.
In vivo(体内研究)
AGI-5198 (450 mg/kg, p.o.) causes 50 to 60% growth inhibition of the tumor growth from human glioma xenografts. Tumors from AGI-5198- treated mice show reduced staining with an antibody against the Ki-67 protein. AGI-5198 does not affect the growth of IDH1 wild-type glioma xenografts.
背景
别名
IDH-C35,AGI5198,AGI 5196
分子式
C27H31FN4O2
CAS号
1355326-35-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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