DDR1-IN-1 dihydrochloride是DDR1受体酪氨酸激酶抑制剂，IC50 值为105 nM，而对 DDR2 的 IC50 为413 nM。
CAS：1780303-76-5
分子式：C30H33Cl2F3N4O3
分子量：625.51
纯度：98%
存储：Store at -20°C

Background:

DDR1-IN-1 dihydrochloride 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)[1]. DDR1|105 nM (IC50)|DDR2|413 nM (IC50)

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[1].

[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.