Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 281 | 现货 | ||
2 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,730 | 现货 | ||
100 mg | ¥ 5,450 | 现货 | ||
200 mg | ¥ 7,650 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 763 | 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 potently inhibits the enzymatic activity of WT MET and a subset of MET mutants found in papillary renal cell carcinoma. The inability of AMG 337 to inhibit the Y1230 and D1228 mutants is likely the result of a disruption of the inactive confirmation of the activation loop in the MET kinase domain. AMG 337 also inhibits cell based HGF-induced MET phosphorylation in PC3 cells with IC50 of 5 nM. AMG 337 inhibits proliferation in MET-dependent cancer cell lines. AMG 337 inhibits signaling through the PI3K and MAPK pathways in MET-amplified gastric cancer cell lines resulting in profound effects on cell proliferation and survival[1]. |
体内活性 | AMG 337 exhibits impressive potency with >90% inhibition of Gab-1 phosphorylation at a dose of 0.75 mg/kg (32 nmol/L free-drug concentration). AMG 337 is well tolerated at continuously administered doses that corresponded with complete MET inhibition for 24 hours, suggesting that AMG 337 has the preClinicalal attributes required to test the role of MET in human cancer[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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 95 mg/mL (204.98 mM)
DMSO: 50 mg/mL (107.88 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.1577 mL | 10.7884 mL | 21.5768 mL | 53.9421 mL |
5 mM | 0.4315 mL | 2.1577 mL | 4.3154 mL | 10.7884 mL | |
10 mM | 0.2158 mL | 1.0788 mL | 2.1577 mL | 5.3942 mL | |
20 mM | 0.1079 mL | 0.5394 mL | 1.0788 mL | 2.6971 mL | |
50 mM | 0.0432 mL | 0.2158 mL | 0.4315 mL | 1.0788 mL | |
100 mM | 0.0216 mL | 0.1079 mL | 0.2158 mL | 0.5394 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
AMG-337 1173699-31-4 Tyrosine Kinase/Adaptors c-Met/HGFR Inhibitor anticancer MKN-45 cell proliferation SNU-5 cells AMG337 SNU-620 phosphorylation AMG 337 inhibit inhibitor