Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
| Catalog No. | Product Name | Size | List Price (US$) | Quantity |
|---|
Price/availability/specifications subject to change without notice. Unless otherwise indicated, our catalog and customized products are for research use only and not intended for human or animal diagnostic or therapeutic use.
Phone: 1-617-401-8149
Fax: 1-617-606-5019
Email: message@sydlabs.com
Or leave a message with a formal purchase
order (PO) Or credit card.
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.
Copyright © 2009-2022 sydlabs.com. All rights reserved.
Use of this website means that you have read, understood, and accepted the Syd Labs Privacy Policy and Terms & Conditions.