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Ivosidenib (AG-120) 是一种口服具有活力的异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 抑制剂,能够使 d-2- hydroxyglutatrate (2-HG) 在体内降低。它具有良好的的安全性和临床活性,具有研究 AML 的潜力。
Ivosidenib (AG-120) 是一种口服具有活力的异柠檬酸脱氢酶 1 的突变体酶 (mIDH1 enzyme) 抑制剂,能够使 d-2- hydroxyglutatrate (2-HG) 在体内降低。它具有良好的的安全性和临床活性,具有研究 AML 的潜力。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 352 | 现货 | |
5 mg | ¥ 788 | 现货 | |
10 mg | ¥ 1,330 | 现货 | |
25 mg | ¥ 2,080 | 现货 | |
50 mg | ¥ 2,990 | 现货 | |
100 mg | ¥ 4,570 | 现货 | |
500 mg | ¥ 9,520 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 973 | 现货 |
产品描述 | Ivosidenib (AG-120) is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2 hG). This may lead to both an induction of cellular differentiation and an inhibition of cellular proliferation in IDH1-expressing tumor cells. |
靶点活性 | IDH1 (R132H):12 nM |
体外活性 | 将携带突变IDH1的Theaflavin-1细胞或初代人AML患者样本用AG-120处理。AG-120治疗降低胞内2-HG水平,抑制生长因子独立的增殖,并在Theaflavin-1 IDH1-R132H细胞中恢复红细胞生成素(EPO)诱导的分化。类似地,通过AG-120药理抑制初代人类爆发细胞中的突变IDH1酶,在体外培养中有效降低胞内2-HG水平并诱导髓系分化[1]。 |
细胞实验 | TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120. (Only for Reference) |
别名 | 艾伏尼布, AG-120 |
分子量 | 582.96 |
分子式 | C28H22ClF3N6O3 |
CAS No. | 1448347-49-6 |
Smiles | Fc1cncc(c1)N([C@H](C(=O)NC1CC(F)(F)C1)c1ccccc1Cl)C(=O)[C@@H]1CCC(=O)N1c1cc(ccn1)C#N |
密度 | 1.51 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 100 mg/mL (171.54 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (85.77 mM) | ||||||||||||||||||||||||||||||||||||||||
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