1429617-90-2

DDR1 Inhibitor 7rh is a small potent kinase inhibitor of discoidin domain receptor-1 (DDR1). It inhibits the tumorigenicity of nasopharyngeal carcinoma (NPC) cells. DDR1 Inhibitor 7rh prevents the proliferation, invasion and adhesion of cancer cells.

DDR1 Inhibitor 7rh is an orally available, potent, ATP-competitive DDR1-selective inhibitor with in vitro and in vivo anti-cancer efficacy. Compound 7rh is a potent, high affinity (Kd =0.6 nM), ATP-competitive inhibitor against discoidin domain-containing receptor 1 (DDR1; IC50 = 6.8 nM, [ATP] = 100 nM) with significantly reduced potency toward 455 other kinases, including DDR2, Bcr-abl, and c-Kit (IC50 = 101.4 nM, 355 nM and >10 μM, respectively). Inhibitor 7rh reduces DDR1 expression/phosphorylation and downstream signaling in a dose-dependent manner (0.1-2 μM; NCI-H23 NSCLCs), effectively suppressing human cancer cells proliferation (IC50 from 38 nM/K562 to 2.98 μM/NCI-H460) and colony formation (IC50 = 0.56 μM/NCI-H23). Inhibitor 7rh is orally availabe in rats and mice (T1/2 = 15.53 h; Tmax = 4.25 h; Cmax = 1867.5 μg/L, F = 67.4%; 25 mg/kg; rats) and displays in vivo efficacy against Kras (LSLG12Vgeo) tumor growth in mice (50 mg/kg/day p.o.).

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