BAY-1436032
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CAS No. | 1803274-65-8 | Cat. No. | BCP18989 |
Name | BAY-1436032 | ||
Synonyms | BAY 1436032;BAY1436032; | ||
SMILES | |||
Chemical Name | |||
Formula | C26H30F3N3O3 | M. Wt | 489.53 |
Purity | 98% | Storage | Store at 4-8°C |
Description | BAY-1436032 is a potent, selective and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). 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 2-HG release (nanomolar 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 2-HG was observed in vitro accompanied by differentiation and maturation of mIDH1 tumor cells. Furthermore, BAY 1436032 showed a favourable selectivity profile against wtIDH1/2 and a large panel of off-targets in vitro. |
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