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:
c-Met/HGFR |
体内研究:
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. |
参考文献:
1.De Bacco F, et al. J Natl Cancer Inst. 2011 Apr, 103(8), 645-661. 2.Torti D, et al. Int J Cancer. 2012, 130(6), 1357-1366. |
溶解性:
H2O:<1 mg/mL Ethanol:<1 mg/mL DMSO:35 mg/mL (92.8 mM) |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.65 ml |
13.25 ml |
26.501 ml |
5 mM |
0.53 ml |
2.65 ml |
5.3 ml |
10 mM |
0.265 ml |
1.325 ml |
2.65 ml |
50 mM |
0.053 ml |
0.265 ml |
0.53 ml |
|
注意: |
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