A potent and selective inhibitor of mutant IDH1 (IC50s = 27

IDH305 – 1 mg

Brand:
Cayman
CAS:
1628805-46-8
Storage:
-20
UN-No:
Non-Hazardous - /

IDH305 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively).{40314} It reduces R-2-hydroxyglutarate (2-HG) production, a marker of mutant IDH1 activity, and inhibits growth of MCF-10A-IDH1R132H/+ cells in a concentration-dependent manner but has no effect on HCT116 cells expressing mutant IDH2. IDH305 (200 mg/kg) reduces the concentration of tumor 2-HG in an HCT116-IDH1R132H/+ mouse xenograft model. It also suppresses 2-HG production and reduces tumor progression in an HMEX2838-IDH1R132C patient-derived melanoma mouse xenograft model when administered at a dose of 300 mg/kg.  

 

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SKU: 24107 - 1 mg Category:

Description

A potent and selective inhibitor of mutant IDH1 (IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively); reduces 2-HG production and inhibits growth of MCF-10A-IDH1R132H/+ cells in a concentration-dependent manner; reduces concentration of tumor 2-HG in an HCT116-IDH1R132H/+ mouse xenograft model (200 mg/kg); suppresses 2-HG production and reduces tumor progression in an HMEX2838-IDH1R132C patient-derived melanoma mouse xenograft model (300 mg/kg),

Formal name: (4R)-4-[(1S)-1-fluoroethyl]-3-[2-[[(1S)-1-[4-methyl-2′-(trifluoromethyl)[3,4′-bipyridin]-6-yl]ethyl]amino]-4-pyrimidinyl]-2-oxazolidinone

Synonyms: 

Molecular weight: 490.5

CAS: 1628805-46-8

Purity: ≥98%

Formulation: A crystalline solid

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

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