IDH1 Inhibitor 1 |
| カタログ番号GC65554 |
IDH1 インヒビター 1 は、IDH1R132H、IDH1R132C、および IDH1WT の IC50 がそれぞれ 0.021 μM、0.045 μM、および 2.52 μM である、強力で、経口で生物学的に利用可能な、脳浸透性かつ選択的な突然変異 IDH1 インヒビターです。抗がん作用。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2234285-81-3
Sample solution is provided at 25 µL, 10mM.
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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].
IDH1 Inhibitor 1 (Compound 19) inhibits cellular HCT116-IDH1R132H/+ with an IC50 of 0.039 μM[1].
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].
[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.
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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