| 产品描述： | NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively. |
| 靶点： |
IC50: 10.3 nM (AXL), 48 nM (MET);Apoptosis; c-Met/HGFR; TAMReceptor |
| 体外研究： |
NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.The expression and activity of AXL is significantly increased in HCC827/ER cells, and NPS-1034 treatment effectively inhibits its tyrosine phosphorylation. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET (phosphorylated MET), with IC50 values of 112.7 and 190.3 nmol, respectively. In contrast, NPS-1034 inhibits AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cell viability with IC50 values ranging from 1 μmol to more than 10 μmol. MET phosphorylation is dramatically decreased after treatment with NPS-1034 in the MKN45 cells, but not in the MKN28 cells. NPS-1034 inhibits hepatocyte growth factor (HGF)-stimulated MET autophosphorylation (Y1234/1235) in the AGS and MKN1 cell lines with IC50 values of <10 and <50 nmol, respectively. HGF-induced MET phosphorylation is completely inhibited by 50 nmol NPS-1034. |
| 体内研究： |
NPS-1034 inhibits tumor proliferation, which highly expresses p-MET. NPS-1034 treatment induces a clear decrease in the vascularization of the tumors. The expression of alpha-smooth muscle actin (α-SMA) is decreased in the tumor sections of mice treated with NPS-1034. NPS-1034-treated mice show virtually no weight loss, indicating that NPS-1034 is generally well tolerated. |
| 参考文献： |
1. Rho JK, et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res. 2014 Jan 1;74(1):253-62.
2. Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2014 Jun;32(3):389-99. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20°C |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.813 ml |
9.065 ml |
18.131 ml |
| 5 mM |
0.363 ml |
1.813 ml |
3.626 ml |
| 10 mM |
0.181 ml |
0.907 ml |
1.813 ml |
| 50 mM |
0.036 ml |
0.181 ml |
0.363 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京