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AMG-337 是有效的、ATP 竞争性的、高度选择性的MET 激酶抑制剂,IC50 < 5 nM。
AMG-337 是有效的、ATP 竞争性的、高度选择性的MET 激酶抑制剂,IC50 < 5 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 266 | 现货 | |
5 mg | ¥ 619 | 现货 | |
10 mg | ¥ 981 | 现货 | |
25 mg | ¥ 1,970 | 现货 | |
50 mg | ¥ 2,870 | 现货 | |
100 mg | ¥ 4,530 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 633 | 现货 |
产品描述 | AMG-337 is an effective and highly specific ATP-competitive MET kinase inhibitor. In enzymatic assays, AMG-337(AMG337) inhibits MET kinase activity (IC50: < 5 nM). |
靶点活性 | MET kinase:< 5 nM |
体外活性 | AMG 337有效抑制WT MET的酶活性及乳头状肾细胞癌中一部分MET突变体。AMG 337无法抑制Y1230和D1228突变体,这可能是因为MET激酶域激活回路非活性构型被破坏所致。此外,AMG 337还能抑制基于细胞的HGF诱导的PC3细胞中MET磷酸化,IC50为5 nM。AMG 337抑制MET依赖的癌细胞系增殖,并在MET扩增的胃癌细胞系中抑制通过PI3K和MAPK途径的信号传导,从而显著影响细胞增殖与生存[1]。 |
体内活性 | AMG 337显示出卓越的效力,在0.75 mg/kg (32 nmol/L自由化合物浓度)的剂量下对Gab-1磷酸化的抑制率超过90%。AMG 337在与完全MET抑制相对应的持续给药剂量下良好耐受,连续24小时,表明AMG 337具备测试MET在人类癌症中作用所需的临床前属性[1]。 |
细胞实验 | To evaluate the effect of AMG 337 on viability, cells are seeded in 96-well plates at an optimal density to ensure proliferation throughout the duration of the experiments. Cells are treated for 72 hours with a 10-point, 3-fold, serial dilution of AMG 337 using a top concentration of 3 mmol/L. Viability is measured with the CellTiter-Glo Luminescent Cell Viability Assay.(Only for Reference) |
别名 | AMG337 |
分子量 | 463.46 |
分子式 | C23H22FN7O3 |
CAS No. | 1173699-31-4 |
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: 95 mg/mL (204.98 mM) DMSO: 50 mg/mL (107.88 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
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