1229611-73-7

LCRF-0004 is a potent and selective RON receptor tyrosine kinase inhibitor. The RON receptor tyrosine kinase has been identified as an important mediator of KRAS oncogene addiction and is overexpressed in the majority of pancreatic cancers. Preclinical studies show that inhibition of RON function decreases pancreatic cancer cell migration, invasion, and survival and can sensitize pancreatic cancer cells to chemotherapy. RON receptor tyrosine kinase is a potential as a therapeutic target.

LCRF-0004 is a potent inhibitor of RON kinase, with the IC50 value of 10 nM. and a surprising result is also obtained regarding its c-Met inhibitory activity, with the IC50 value of 12 nM. LCRF-0004 plays an important role in cancer research[1].

[1] Stéphane L Raeppel, et al. Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor. Bioorg Med Chem Lett. 2015 Jun 15;25(12):2527-31. DOI:10.1016/j.bmcl.2015.04.056