BAY-1436032
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| Catalog No. | APIM050314 |
|---|---|
| Product Name | BAY-1436032 |
Description
Background Information:
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.
Reference:
1. Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA, Volume. 76 Issue. 14 Supplement, pp. 2645.
2. Michael Heuser, et al, Pan-Mutant-IDH1 Inhibitor Bay-1436032 Is Highly Effective Against Human IDH1 Mutant Acute Myeloid Leukemia In Vivo, Blood 2016 128:745.
3. A. Chaturvedi, et al, Pan-mutant-IDH1 inhibitor BAY1436032 is highly effective against human IDH1 mutant acute myeloid leukemia in vivo, Leukemia (31 January 2017) | doi:10.1038/leu.2017.46.
APIM050314: BAY-1436032
CAS No.: 1803274-65-8.
Molecular Formula: C26H30F3N3O3.
Molecular Weight: 489.5 (refer to Certificate of Analysis, batch-specific).
Purity: >99.5% Chem and Optical purity (by achiral HPLC and chiral HPLC).
QC: HPLC-MS, 1H-NMR, Chiral HPLC, and Elemental Analysis Report.
Solubility: Refer to Certificate.
Storage: Refer to Certificate.
