IDH305 |
رقم الكتالوجGC18423 |
IDH305 هو مثبط فعال وانتقائي لإنزيم الأيزوسيترات دهايدروجيناز 1 المتحور (IDH1؛ IC50s = 27، 28، و6،140 نانومتر لـ IDH1R132H المكونة بالتقارب ، IDH1R132C ، و IDH1 البرية على التوالي).
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Cas No.: 1628805-46-8
Sample solution is provided at 25 µL, 10mM.
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.
Review for IDH305
Average Rating: 5
(Based on Reviews and 18 reference(s) in Google Scholar.)Review for IDH305
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