| 名称 | JNJ-38877605 |
| 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. |
| 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. |
| 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. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 6 mg/mL (15.9 mM), Sonication is recommended.
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| 关键字 | c-Met/HGFR | JNJ-38877605 | Inhibitor | inhibit | JNJ38877605 | JNJ 38877605 |
| 相关产品 | Cabozantinib | Capmatinib 2HCl | SGI-7079 | (±)-Norcantharidin | L-Ascorbic acid 2-phosphate trisodium | Crizotinib | Amuvatinib | Norcantharidin | Cabozantinib S-malate | Capmatinib xHCl | Bacitracin Zinc | Capmatinib |
| 相关库 | 高选择性抑制剂库 | 经典已知活性库 | 膜蛋白靶向化合物库 | 激酶抑制剂库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
