An inhibitor of mutant IDH1 (IC50s = 9

GSK864 – 500 µg

Brand:
Cayman
CAS:
1816331-66-4
Storage:
-20
UN-No:
Non-Hazardous - /

GSK864 is an allosteric inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 9, 15, and 17 nM for IDH1 mutants R132C, R132H, and R132G, respectively).{29821} It is moderately selective for mutant IDH1 over wild-type IDH1 and IDH2 mutants/wild-type. GSK864 causes a dose-dependent reduction in 2-hydroxyglutarate and overcomes the block of differentiation in acute myeloid leukemia (AML) cells expressing mutant IDH1.{29821} It reduces the number of leukemic blasts in mice with AML xenografts.{29821} See the Structural Genomics Consortium (SGC) website for more information.  

 

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Description

An inhibitor of mutant IDH1 (IC50s = 9, 15, and 17 nM for IDH1 mutants R132C, R132H, and R132G, respectively); causes a dose-dependent reduction in 2-hydroxyglutarate and overcomes the block of differentiation in AML cells expressing mutant IDH1

Formal name: (S)-1-(4-fluorobenzyl)-N3-(4-methoxy-3,5-dimethylphenyl)-7-methyl-5-(1H-pyrrole-2-carbonyl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridine-3,7-dicarboxamide

Synonyms: 

Molecular weight: 558.6

CAS: 1816331-66-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer||Research Area|Cell Biology|Mitochondrial Biology

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