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| | IDH1 Inhibitor 1 Basic information |
| Product Name: | IDH1 Inhibitor 1 | | Synonyms: | IDH1 Inhibitor 1;2-Oxazolidinone, 4-(fluoromethyl)-3-[2-[[(1S)-1-[1-[4-(trifluoromethyl)phenyl]-1H-imidazol-4-yl]ethyl]amino]-4-pyrimidinyl]-, (4R)-;IDH-1 Inhibitor 1,IDH1 Inhibitor 1 | | CAS: | 2234285-81-3 | | MF: | C20H18F4N6O2 | | MW: | 450.39 | | EINECS: | | | Product Categories: | | | Mol File: | 2234285-81-3.mol |  |
| | IDH1 Inhibitor 1 Chemical Properties |
| storage temp. | 4°C, away from moisture and light | | form | Solid | | color | White to off-white |
| | IDH1 Inhibitor 1 Usage And Synthesis |
| Uses | IDH1 Inhibitor 1 is a potent, orally bioavailable, brain-penetrant and selective mutant IDH1 inhibitor with IC50s of 0.021 μM, 0.045 μM, and 2.52 μM for IDH1R132H, IDH1R132C, and IDH1WT, respectively[1]. Anticancer activity[1]. | | in vivo | IDH1 Inhibitor 1 (Compound 19) inhibits 2-hydroxyglutarate (2-HG) production in a preclinical xenograft tumor model. IDH1 Inhibitor 1 is also profiled in a patient-derived IDH1 mutant HCT116-IDH1R132H/+ mechanistic xenograft tumor model in mice to evaluate in vivo inhibition of 2-HG production. IDH1 Inhibitor 1, dosed orally at 150 mg/kg, inhibits new 2-HG production[1]. | | References | [1] Zhao Q, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Orally Bioavailable and Brain Penetrant Mutant IDH1 Inhibitors. ACS Med Chem Lett. 2018 Jun 11;9(7):746-751. DOI:10.1021/acsmedchemlett.8b00182 |
| | IDH1 Inhibitor 1 Preparation Products And Raw materials |
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