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  • DDR1-IN-1 dihydrochloride
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DDR1-IN-1 dihydrochloride

DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2.

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  • 货号: ajce55886
  • CAS: 1780303-76-5
  • 别名:
  • 分子式: C30H33Cl2F3N4O3
  • 分子量: 625.51
  • 纯度: >98%
  • 溶解度: Soluble in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, about 3-fold selectivity over DDR2.


In U2OS cells, DDR1-IN-1 inhibits basal DDR1 autophosphorylation with EC50 of 86 nM, and demonstrates stronger inhibition of DDR1 autophosphorylation in the absence of collagen stimulation. In a panel of different cancer cell lines that possess DDR1 gain-of-function mutations and/or overexpression, DDR1-IN-1, dose not inhibit proliferation below a concentration of 10 μM, while GSK2126458 potentiates the antiproliferative activity of DDR1-IN-1. [1]


[1] Kim HG, et al. ACS Chem Biol. 2013, 8(10), 2145-2150.

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