Vorasidenib

An inhibitor of mutant IDH1 and IDH2

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库存: 现货

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数量
2mg

￥912.00

730.00

- +
5mg

￥1575.00

1260.00

- +
10mg

￥2562.00

2050.00

- +
50mg

￥7612.00

6090.00

- +
100mg

￥11450.00

9160.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajci23002
CAS: 1644545-52-7
别名: PVM/MA共聚物,AG-881
分子式: C14H13ClF6N6
分子量: 414.74
纯度: >98%
溶解度: DMSO : ≥ 125 mg/mL (301.39 mM);Water : < 0.1 mg/mL (insoluble)
储存: Store at -20°C
库存: 现货

Background

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].

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.