Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ38877605 是 ATP 竞争性 c-Met 抑制剂 (IC50:4 nM),对c-Met 的抑制性比对其它 200 种酪氨酸和丝氨酸-苏氨酸激酶的抑制性高 600 倍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 475 | 现货 | ||
10 mg | ¥ 774 | 现货 | ||
50 mg | ¥ 2,268 | 现货 | ||
100 mg | ¥ 3,996 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 475 | 现货 |
产品描述 | JNJ-38877605 is an ATP-competitive c-Met inhibitor (IC50: 4 nM), 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. |
靶点活性 | c-Met:4 nM |
体外活性 | JNJ-38877605 shows more than 600-fold selectivity for c-Met compared with more than 200 other diverse tyrosine and serine-threonine kinases and also potently inhibits HGF-stimulated and constitutively activated c-Met phosphorylation in vitro. In EBC1, GTL16, NCI-H1993, and MKN45 cells, JNJ-38877605 (500 nM) leads to a significant reduction of phosphorylation of Met and RON, another key player in invasive growth. A recent study shows that JNJ-38877605 is involved in modulating secretion of IL-8, GROa, uPAR and IL-6 in GTL16 cells. |
体内活性 | In mice bearing established GTL16 xenografts, JNJ-38877605 (40 mg/kg/day, p.o., total 3day) results in a statistically marked decrease in the plasma levels of human IL-8 (0.150-0.050 ng/mL) and GROα (0.080-0.030 ng/mL). While concentrations of uPAR in the blood become reduced to more than 50% at the same dose. |
动物实验 | Animal Models: GTL16 cells are inoculated subcutaneously into the right posterior flank (or both right and left posterior flanks,for determination of uPAR and IL-6) of 6-week-old immuno-deficient nu/nu female mice on Swiss CD1 background. Formulation: JNJ-38877605 is dissolved in PBS. Dosages: ≤40 mg/kg/day. Administration: Administered via p.o. |
分子量 | 377.35 |
分子式 | C19H13F2N7 |
CAS No. | 943540-75-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 35 mg/mL (92.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6501 mL | 13.2503 mL | 26.5006 mL | 66.2515 mL |
5 mM | 0.53 mL | 2.6501 mL | 5.3001 mL | 13.2503 mL | |
10 mM | 0.265 mL | 1.325 mL | 2.6501 mL | 6.6251 mL | |
20 mM | 0.1325 mL | 0.6625 mL | 1.325 mL | 3.3126 mL | |
50 mM | 0.053 mL | 0.265 mL | 0.53 mL | 1.325 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。
JNJ-38877605 943540-75-8 Tyrosine Kinase/Adaptors c-Met/HGFR Inhibitor inhibit JNJ38877605 JNJ 38877605 inhibitor