| 產(chǎn)品描述： | NVP-BVU972 is a selective and potent Met inhibitor with IC50 of 14 nM. |
| 靶點(diǎn)： |
c-Met/HGFR |
| 體內(nèi)研究： |
NVP-BVU972有效抑制MET基因擴(kuò)散的細(xì)胞系GTL-16,MKN-45和EBC-1的生長(zhǎng),IC50分別為66,82和32 nM。NVP-BVU972有效抑制MET激酶,而對(duì)其他激酶（包括最密切相關(guān)的激酶）RON抑制作用很低,IC50>1000 nM。NVP-BVU972抑制GTL-16細(xì)胞中組成型MET磷酸化,抑制A549細(xì)胞中HGF刺激的MET磷酸化,IC50分別為7.3和 22 nM。NVP-BVU972作用于表達(dá)野生型TPR-MET的BaF3細(xì)胞,劑量依賴性降低TPR-MET磷酸化。 |
| 細(xì)胞實(shí)驗(yàn)： |
BaF3 cells containing TPR-MET or various mutants thereof are grown in RPMI 1640 medium containing 10% fetal calf serum. For maintenance of parental BaF3 cells the medium is additionally supplemented with 10 ng/mL interleukin-3 (IL-3). For proliferation assays, BaF3 cells are seeded on 96-well-plates in triplicates at 104 cells per well and incubated with various concentrations of NVP-BVU972 for 72 hours followed by quantification of viable cells using a resazurin sodium salt dye reduction readout. IC50 values are determined with the XLFit Excel Add-In using a 4-parameter dose response model.(Only for Reference) |
| 參考文獻(xiàn)： |
1. Tiedt R, et al. Cancer Res. 2011, 71(15), 5255-5264. |
| 溶解性： |
Soluble in DMSO、Ethanol |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.938 ml |
14.689 ml |
29.379 ml |
| 5 mM |
0.588 ml |
2.938 ml |
5.876 ml |
| 10 mM |
0.294 ml |
1.469 ml |
2.938 ml |
| 50 mM |
0.059 ml |
0.294 ml |
0.588 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