Welcome visitor Log In - or - Register
(
0 items /
$0.00
)
View Cart
Check Out
four ways
Quick Search:
Skip Navigation LinksHome > IDH (Isocitrate Dehydrogenase) Inhibitors > Mutant-IDH1 Inhibitor > BAY-1436032
BAY-1436032
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.
Catalog NO: CT-BAY143
Synonym: BAY1436032
CAS NO: 1803274-65-8
Mol. Formula: C26H30F3N3O3
MW: 489.5 (refer to Certificate of Analysis, batch-specific)
** in vivo Quality Material. 99.9% chemically and optically pure by achiral and chiral HPLCs. A milk-white powder. Clean and impeccable. Bulk stock! Same day shipping.
Northeast Business Center, 7301 E. 90th Street, Suite 117,Indianapolis, IN 46256, USA;
Tel: 317-598-0828, Toll-free: 1-877-343-6578 (US and Canada only);Fax: 317-598-0835; info@chemietek.com
Copyright © 2014 Chemietek. All Rights Reserved.