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Axon 3863

CAS [1803274-65-8]

MF C26H30F3N3O3
MW 489.53

  • Purity: 99%
  • Optical purity: 99%
  • Soluble in DMSO



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. BBB penetrant.

KEYWORDS: BAY-1436032 | Supplier | Mutant Isocitrate Dehydrogenase 1 (mIDH1) inhibitor | BAY1436032 | BAY 1436032 | CT-BAY143 | CAS [1803274-65-8] | Isocitrate | IDH | Inhibitor | Enzymes

Highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1)

Chemical name

3-(2-(4-(Trifluoromethoxy)phenylamino)-1-((1R,5R)-3,3,5-trimethylcyclohexyl)-1H-benzo[d]imidazol-5-yl)propanoic acid

Source information

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Parent CAS No.


The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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