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BAY-1436032 is a highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). Optically pure BAY-1436032 is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displayed potent inhibition of “oncometabolite” 2-hydroxyglutarate (2-HG) release (nM range) in patient derived and engineered cell lines expressing different IDH1 mutants. In line with the proposed mode of action, a concentration-dependent lowering of 2HG was observed in vitro accompanied by differentiation of maturation of mIDH1 tumor cells. It also showed a favorable selective profile against wIDH1/2 and a large panel of off-target proteins. Demonstrated a single agent in vivo efficacy in mIDH1 patient derived glioma and intrahepatic cholangiocarcinoma solid tumor model. It is highly effective against human IDH1 mutant acute myeloid leukemia in vivo (ref 2&3). BBB penetrant.
Catalog NO: CT-BAY143
Synonym: BAY1436032
CAS NO: 1803274-65-8
Mol. Formula: C26H30F3N3O3
MW: 489.5 (refer to Certificate of Analysis, batch-specific)
** in vivo Quality Material. 99.9% chemically and optically pure by achiral and chiral HPLCs. A milk-white powder. Clean and impeccable. Bulk stock! Same day shipping.