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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 | In stock | |
| 5 mg | ¥ 619 | In stock | |
| 10 mg | ¥ 981 | In stock | |
| 25 mg | ¥ 1,970 | In stock | |
| 50 mg | ¥ 2,870 | In stock | |
| 100 mg | ¥ 4,530 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 633 | In stock |
AMG-337 相关产品
| 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:< 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 |
| Smiles | COCCOc1cnc2ccn([C@H](C)c3nnc4c(F)cc(cn34)-c3cnn(C)c3)c(=O)c2c1 |
| 密度 | 1.44 g/cm3 (Predicted) |
| 颜色 | White |
| 物理性状 | Solid |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | Ethanol: 95 mg/mL (204.98 mM), Sonication is recommended. DMSO: 50 mg/mL (107.88 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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DMSO/Ethanol
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