An inhibitor of mutant IDH1 (IC50s = 42

Mutant IDH1-IN-1 – 50 mg

Brand:
Cayman
CAS:
1355326-21-4
Storage:
-20
UN-No:
Non-Hazardous - /

Mutant IDH1-IN-1 is a selective inhibitor of the cancer-associated enzyme mutant isocitrate dehydrogenase 1 (IDH1; Item No. 14131) with IC50 values of 42, 4, and 80 nM for homozygous R132H and R132C mutant and heterozygous R132H wild-type enzymes, respectively, for converting α-ketoglutarate (α-KG) to 2-hydroxyglutaric acid (2-HG).{37556} It is selective for IDH1 mutant conversion of α-KG to 2-HG over homozygous wild-type enzyme conversion of isocitrate to α-KG (IC50 = 1,998 nM) and over IDH2 (IC50s = >10,000 nM). Mutant IDH1-IN-1 inhibits 2-HG production in vitro (IC50 = 81.5 nM in HEK293 cells expressing IDH1R132H). It allosterically binds to mutant IDH1 in a magnesium-dependent manner.  

 

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Description

An inhibitor of mutant IDH1 (IC50s = 42, 4, and 80 nM for IDH1R132H/R132H, IDH1R132C/R132C, and IDH1R132H/WT, respectively, for conversion of α-KG to 2-HG); selective for IDH1 mutant conversion of α-KG to 2-HT over IDH1WT/WT conversion of isocitrate to α-KG (IC50 = 1,998 nM) and over IDH2 (IC50s = >10,000 nM); inhibits 2-HG production in vitro (IC50 = 81.5 nM),

Formal name: N-[2-(cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-1H-benzimidazole-1-acetamide

Synonyms: 

Molecular weight: 498.6

CAS: 1355326-21-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Endocrinology & Metabolism

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