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DDR1-IN-1 dihydrochloride
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
DDR1-IN-1 dihydrochloride图片
CAS NO:1780303-76-5

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 No.1780303-76-5
Canonical SMILESCC1=C(C=C(C=C1)NC(C2=CC=C(C(C(F)(F)F)=C2)CN3CCN(CC3)CC)=O)OC4=CC(C5)=C(C=C4)NC5=O.Cl.Cl
分子式C30H33Cl2F3N4O3
分子量625.51
溶解度Soluble in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.

 
 
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