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MCE 国际站:Vorasidenib
CAS:1644545-52-7
品牌:MedChemExpress (MCE)
存储条件:Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
生物活性:Vorasidenib (AG-881) 是一种可口服的脑渗透第二代双重突变型异柠檬酸脱氢酶 1 和 2 (mIDH1/2) 抑制剂。 Vorasidenib (AG-881) 对 (D)-2-hydroxyglutarate (D-2-HG) 具有纳摩尔抑制作用,IC50 范围为 0.04~22 nM IDH1 R132C、IDH1 R132G、IDH1 R132H 和 IDH1 R132S 以及 7~14 nM 对抗 IDH2 R140Q 和 130 nM 对抗 IDH2 R172K[1][2]。 IC50 和目标:IC50:0.04~22 nM(IDH1 R132C、IDH1 R132G、IDH1 R132H、IDH1 R132S)、7~14 nM(IDH2 R140Q)、130 nM(IDH2 R172K)[2]
体外:Vorasidenib 对人胶质母细胞瘤 U-87 MG pLVX-IDH2 R140Q-neo、纤维肉瘤 HT-1080 和神经球 TS603 细胞具有很强的抗增殖活性,IC50 均小于 50 nM[2 ]。
热销产品:1,2-Cyclohexanedione | Pelitinib | Grepafloxacin (hydrochloride) | Propranolol-d7 (ring-d7) | Neohesperidin dihydrochalcone | 1,3-Butanediol | BCECF | Myricetin 3-O-galactoside | 7-Methylxanthine | Tetrabutylammonium (fluoride)
研究领域:Metabolic Enzyme/Protease
作用靶点:Isocitrate Dehydrogenase (IDH)
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides
参考文献:[1]. Fujii T, et al. Targeting isocitrate dehydrogenase (IDH) in cancer. Discov Med. 2016 May;21(117):373-80.[2]. Ma T, et al. Inhibitors of Mutant Isocitrate Dehydrogenases 1 and 2 (mIDH1/2): An Update and Perspective. J Med Chem. 2018 Oct 25;61(20):8981-9003.
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