Vorasidenib-AG-881-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVorasidenibCat. No.: HY-104042CAS No.: 1644545-52-7Synonyms: AG-881分式: CHClFN分量: 414.74作靶點: Isocitrate Dehydrogenase (IDH)作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體

2、外實驗 DMSO : 125 mg/mL (301.39 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (5.02 mM); Suspended solution; Need ultrasonic2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (5.02 mM); Suspended solution; Need ult

3、rasonic3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (5.02 mM); Clear solution; Need warmingBIOLOGICAL ACTIVITY物活性 Vorasidenib (AG-881)種可服的、腦滲透的第代突變體異檸檬酸脫氫酶 1 和 2 (mIDH1/2) 雙重 抑制劑，其以納爾抑制 D-2-HG，對 IDH1 R132C、IDH1 R132G、IDH1 R132H、IDH1 R132S 的 IC50 值為 0.0422nM，對 IDH2 R140Q 值為 714 nM，對 IDH2

4、 R172K 的值為 130 nM 1 2。IC50 & Target IC50: 0.0422 nM (IDH1 R132C, IDH1 R132G, IDH1 R132H, IDH1 R132S), 714 nM (IDH2 R140Q), 130 nM(IDH2 R172K) 2體外研究 Vorasidenib has strong antiproliferative activity against human glioblastoma U-87 MG pLVX-IDH2 R140Q-neo, fibrosarcoma HT-1080 and neurosphere TS603 cel

5、ls, all with IC50s of less than 50 nM 2.REFERENCES1. 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 Oct25;61(20):8981-9003.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792; 021