IDH889 |
Katalog-Nr.GC38640 |
IDH889 ist ein oral verfÜgbarer, in das Gehirn eindringender, allosterischer und mutantenspezifischer Inhibitor der Isocitratdehydrogenase 1 (IDH1). IDH889 hat eine starke SelektivitÄt fÜr IDH1 R132*-Mutationen mit IC50-Werten von 0,02 μM, 0,072 μM und 1,38 μM fÜr IDH1R132H, IDH1R132C bzw. IDH1wt. IDH889 zeigt eine starke zellulÄre Hemmung der Produktion von R-2-Hydroxyglutarat (2-HG) mit einem IC50 von 0,014 μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1429179-07-6
Sample solution is provided at 25 µL, 10mM.
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM[1].
[1]. Levell JR, et al. Optimization of 3-Pyrimidin-4-yl-oxazolidin-2-ones as Allosteric and Mutant Specific Inhibitors of IDH1. ACS Med Chem Lett. 2016 Dec 16;8(2):151-156.
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