Product Name: BAY-1436032

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CAT#: A-6039


BAY-1436032 Chemical Structure BAY-1436032 chemical structure

IUPAC/Chemical name: CHEMFIELD

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Biological Activity
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. BBB penetrant.
Technical Data
M.Wt:      489.5
Formula:     C26H30F3N3O3
CAS#: 1803274-65-8
Purity: >99 % by chiral HPLC
Storage Conditions: Room temperature for short term or -20ºC for 3 years.