Vorasidenib

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Vorasidenib

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1644545-52-7

包装与价格：

包装	价格(元)
2mg	询价
5mg	询价
10mg	询价
50mg	询价
100mg	询价

Vorasidenib (AG-881) 是一种可口服的、脑渗透性的第二代双突变异柠檬酸脱氢酶 1 和 2 (mIDH1/2) 抑制剂。 Vorasidenib (AG-881) 对 (D)-2-羟基戊二酸 (D-2-HG) 具有纳摩尔抑制作用，对 IDH1 R132C、IDH1 R132G、IDH1 R132H 和 IDH1 R132S 和 7~14 的 IC50 范围为 0.04~22 nM nM 针对 IDH2 R140Q 和 130 nM 针对 IDH2 R172K。

Cas No.	1644545-52-7
别名	PVM/MA共聚物,AG-881
Canonical SMILES	C[C@@H](NC1=NC(C2=NC(Cl)=CC=C2)=NC(N[C@H](C)C(F)(F)F)=N1)C(F)(F)F
分子式	C₁₄H₁₃ClF₆N₆
分子量	414.74
溶解度	DMSO : ≥ 125 mg/mL (301.39 mM);Water :< 0.1 mg/mL (insoluble)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K[1][2]. Vorasidenib has strong antiproliferative activity against human glioblastoma U-87 MG pLVX-IDH2 R140Q-neo, fibrosarcoma HT-1080 and neurosphere TS603 cells, all with IC50s of less than 50 nM[2]. References: [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.