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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Isocitrate Dehydrogenase (IDH)-Vorasidenib
Vorasidenib

Chemical Structure : Vorasidenib

CAS No.: 1644545-52-7

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Vorasidenib (AG-881, AG 881, AG881)

货号: PC-60534Not For Human Use, Lab Use Only.

Vorasidenib (AG-881) is a potent, oral, brain-penetrant dual inhibitor of mIDH1 and mIDH2 with IC50 of 6 nM and 12 nM for IDH1-R132H and IDH2-R140Q, respectively.

规格 价格 库存 数量
5 mg ￥1280 In stock
10 mg ￥1880 In stock
25 mg ￥2980 In stock
50 mg ￥4980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Vorasidenib (AG-881) is a potent, oral, brain-penetrant dual inhibitor of mIDH1 and mIDH2 with IC50 of 6 nM and 12 nM for IDH1-R132H and IDH2-R140Q, respectively.
Vorasidenib (AG-881) binds both IDH1-R132H and IDH2-R140Q in the same allosteric pocket at the interface of the two monomers.
Vorasidenib (AG-881) (50 mg/kg) inhibits 2-HG levels in an orthotopic grade III mIDH1 glioma model derived from the TS603 neurosphere.
Vorasidenib (AG-881) penetrates the brain of several preclinical species and inhibits 2-HG production in glioma tissue by >97% in an orthotopic glioma mouse model.
Vorasidenib (AG-881) shows for the treatment of several cancers harboring an IDH mutation.

物理化学性质&存储条件

分子量 414.74
分子式 C14H13ClF6N6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

6-(6-chloropyridin-2-yl)-N2,N4-bis((R)-1,1,1-trifluoropropan-2-yl)-1,3,5-triazine-2,4-diamine

参考文献

1. Konteatis Z, et al. ACS Med Chem Lett. 2020 Jan 22;11(2):101-107.
2. Mellinghoff IK, et al. N Engl J Med. 2023 Aug 17;389(7):589-601.
3. Mellinghoff IK, et al. Nat Med. 2023 Mar;29(3):615-622.

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