1628805-46-8IDH305

产品属性：

Cas No.1628805-46-8

别名 N/A

化学名 (4R)-4-[(1S)-1-fluoroethyl]-3-[2-[[(1S)-1-[4-methyl-2'-(trifluoromethyl)[3,4'-bipyridin]-6-yl]ethyl]amino]-4-pyrimidinyl]-2-oxazolidinone

分子式 C23H22F4N6O2

分子量 490.5

溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml,Ethanol:PBS (pH7.2)(1:20): 0.05 mg/ml

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
IDH305 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (IDH1; IC50s = 27, 28, and 6,140 nM for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively). It reduces R-2-hydroxyglutarate (2-HG) production, a marker of mutant IDH1 activity, and inhibits growth of MCF-10A-IDH1R132H/+ cells in a concentration-dependent manner but has no effect on HCT116 cells expressing mutant IDH2. IDH305 (200 mg/kg) reduces the concentration of tumor 2-HG in an HCT116-IDH1R132H/+ mouse xenograft model. It also suppresses 2-HG production and reduces tumor progression in an HMEX2838-IDH1R132C patient-derived melanoma mouse xenograft model when administered at a dose of 300 mg/kg.