1780303-76-5

1780303-76-5 structure
1780303-76-5 structure
  • Name: DDR1-IN-1 dihydrochloride
  • Chemical Name: DDR1-IN-1 dihydrochloride
  • CAS Number: 1780303-76-5
  • Molecular Formula: C30H33Cl2F3N4O3
  • Molecular Weight: 625.51
  • Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Discoidin Domain Receptor
  • Create Date: 2019-06-01 12:07:31
  • Modify Date: 2024-01-13 15:22:38
  • 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].

Name DDR1-IN-1 dihydrochloride
Description 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].
Related Catalog
Target

DDR1:105 nM (IC50)

DDR2:413 nM (IC50)

In Vitro 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].
References

[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.

Molecular Formula C30H33Cl2F3N4O3
Molecular Weight 625.51