WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407343
Description: DDR1-IN-1 is a potent and selective DDR1 inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2. DDR1-IN-1 binds to DDR1 in the 'DFG-out' conformation and inhibits DDR1 autophosphorylation in cells at submicromolar concentrations with good selectivity as assessed against a panel of 451 kinases measured. DDR1-IN-1 provides a useful pharmacological probe for DDR1-dependent signal transduction. The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion.
MedKoo Cat#: 407343
Chemical Formula: C30H31F3N4O3
Exact Mass: 552.2348
Molecular Weight: 552.5982
Elemental Analysis: C, 65.21; H, 5.65; F, 10.31; N, 10.14; O, 8.69
Synonym: DDR1-IN-1; DDR1-IN 1; DDR1-IN1.
IUPAC/Chemical Name: 4-((4-ethylpiperazin-1-yl)methyl)-N-(4-methyl-3-(2-oxoindolin-5-yloxy)phenyl)-3-(trifluoromethyl)benzamide
SMILES Code: FC(C1=CC(C(NC2=CC=C(C(OC3=CC(C4)=C(C=C3)NC4=O)=C2)C)=O)=CC=C1CN5CCN(CC)CC5)(F)F
1: Canning P, Tan L, Chu K, Lee SW, Gray NS, Bullock AN. Structural mechanisms
determining inhibition of the collagen receptor DDR1 by selective and
multi-targeted type II kinase inhibitors. J Mol Biol. 2014 Jun
26;426(13):2457-70. doi: 10.1016/j.jmb.2014.04.014. Epub 2014 Apr 23. PubMed
PMID: 24768818; PubMed Central PMCID: PMC4058747.
2: Kim HG, Tan L, Weisberg EL, Liu F, Canning P, Choi HG, Ezell SA, Wu H, Zhao Z,
Wang J, Mandinova A, Griffin JD, Bullock AN, Liu Q, Lee SW, Gray NS. Discovery of
a potent and selective DDR1 receptor tyrosine kinase inhibitor. ACS Chem Biol.
2013 Oct 18;8(10):2145-50. doi: 10.1021/cb400430t. Epub 2013 Aug 13. Erratum in:
ACS Chem Biol. 2014 Mar 21;9(3):840. PubMed PMID: 23899692; PubMed Central PMCID: