Chemical Name: 4-Ethyl-N-[3-[(4-methyl-1-piperazinyl)methyl]-5-(trifluoromethyl)phenyl]-3-(2-pyrazolo[1,5-a]pyrimidin-6-ylethynyl)benzamide
Biological Activity7rh is a potent and selective DDR1 inhibitor (IC50 = 6.8 nM). Exhibits selectivity for DDR1 over DDR2, Bcr-Abl and c-Kit (IC50 values are 101.4 and 355 nM and > 10 μM, respectively) and a range of other kinases. Inhibits proliferation of cancer cell lines expressing high levels of DDR1 in vitro and suppresses cancer cell invasion, adhesion and tumorigenicity. Orally bioavailable.
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