| 產(chǎn)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. |
| 靶點(diǎn)： |
c-Met/HGFR |
| 體內(nèi)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. |
| 動(dòng)物實(shí)驗(yàn)： |
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. |
| 參考文獻(xiàn)： |
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) |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
北京