IDH305 是一种可口服的、突变选择性和脑渗透性 IDH1 抑制剂，靶向 IDH1 (R132) 突变。 IDH305 对突变 IDH1 亚型与 WT 相比表现出超过 200 倍的选择性（IC50\u003d 27 nM (IDH1R132H)、28 nM (IDH1R132C)、6.14 μM (IDH1WT)）。
| Cas No. | 1628805-46-8 |
| 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 |
| Canonical SMILES | CC(C=C([C@H](C)NC1=NC(N2C(OC[C@]2([H])[C@@H](F)C)=O)=CC=N1)N=C3)=C3C4=CC=NC(C(F)(F)F)=C4 |
| 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. |
m.cnreagent.com