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产品描述： DDR1-IN-1 is a potent and selective DDR1 receptor tyrosine kinase inhibitor with an IC50 of 105 nM; 4-fold less potent for DDR2 (IC50 = 413 nM) |
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靶点：
IC50: 105 nM (DDR1);DiscoidinDomainReceptor(DDR) |
体外研究：
DDR1-IN-1 effectively blocks collagen-induced DDR1 pY513 autophosphorylation in U2OS cells (EC50 = 86.76 nM) with excellent selectivity over a panel of >380 kinases. DDR1-IN-1 inhibits DDR2-mediated MT1-MMP activation in human rheumatoid synovial fibroblasts (RASF) upon collagen stimulation (IC50 < 2.5 μM) and enhances PI3K/mTOR inhibitor GSK2126458 antiproliferation efficacy in SNU-1040 colorectal cancer culture |
参考文献：
1. Kim HG, et al. Discovery of a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol. 2013 Oct 18;8(10):2145-50. |
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溶解性：
soluble in DMSO |
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保存条件：
-20°C |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
1.81 ml |
9.048 ml |
18.097 ml |
| 5 mM |
0.362 ml |
1.81 ml |
3.619 ml |
| 10 mM |
0.181 ml |
0.905 ml |
1.81 ml |
| 50 mM |
0.036 ml |
0.181 ml |
0.362 ml |
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| 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
北京