AZM475271 is a potent and selective inhibitor of Src kinase(IC50 : 5 nM)

AZM475271 demonstrated strong dose-dependent inhibition of Src tyrosine kinase activity in the L3.6pl human pancreatic carcinoma cell line. The IC50 concentration of AZM475271 to inhibit the phosphorylation of c-src, lck, and c-yes was 0.01, 0.03, and 0.08 μmol/L, respectively, in comparison with an IC50 of 0.7 μmol/L AZM475271 to inhibit KDR [2]. Maximum reduction of Src kinase activity was observed after incubation for 4 hours with ≥5 μmol/L.

Treatment with gemcitabine or AZM475271 alone did not significantly change animal weight [2]. In vivo: Tumors appeared to be palpable at day 14 after tumor cell injection in all animals except mice treated with both AZM475271 and gemcitabine, in which the earliest possible palpation of the tumors was at day 17 after tumor cell injection.