AGI5198 1355326-35-0

Name: AGI5198 1355326-35-0abs810560
Brand: absin
Price: 375 CNY
Availability: InStock

簡要描述：AGI5198 1355326-35-0
AGI-5198 is the first highly potent and selective inhibitor of IDH1 R132H/R132C mutants with IC50 of 0.07 μM/0.16 μM.

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詳細介紹

品牌	absin	CAS	1355326-35-0
分子式	C27H31FN4O2	純度	＞98%
分子量	462.56	貨號	abs810560
供貨周期	現貨	主要用途	is the first highly potent and selective
應用領域	化工,生物產業,農林牧漁,制藥/生物制藥,綜合

AGI5198 1355326-35-0

產品描述
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.
純度	>98%
儲存/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
別名	IDH-C35,AGI5198,AGI 5196
外觀	Powder
可溶性/溶解性	DMSO 24 mg/mL (51.88 mM) Ethanol 14 mg/mL (30.26 mM)
生物活性
靶點	Isocitrate Dehydrogenase (IDH)
In vitro(體外研究)	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(體內研究)	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.