| Identification | Back Directory | [Name]
IDH1 Inhibitor 1 | [CAS]
2234285-81-3 | [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)- | [Molecular Formula]
C20H18F4N6O2 | [MDL Number]
MFCD31813679 | [MOL File]
2234285-81-3.mol | [Molecular Weight]
450.39 |
| Hazard Information | Back Directory | [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 |
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| Company Name: |
MedChemExpress
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| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
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