AZD7507 is a CSF-1R inhibitor with an IC50 of 32 nM. AZD7507 has antitumor activity.

CSF1R:32 nM, Nav1.5:26 μM, ERG (human):>30 μM

AZD7507 inhibits the proliferation of 3T3 cells engineered to express CSF-1R and stimulated with CSF-1. It shows inhibitory activity against hERG and NaV1.5, with IC50s of >30 and 26 μM[1].

Xenografted mice were given liposomal clodronate (Lipclod) to selectively deplete phagocytic macrophages; AZD7507 to inhibit the activation of CSF receptor 1 (CSFR1), thereby preventing monocyte differentiation into macrophages; or appropriate vehicle alone[2]. In Lipclod-, GW2580-, and AZD7507-treated mice, we observed a significant decrease the number of CD68+ macrophages in the xenografted. Mice with CC-LP-1 and SNU-1079, but not WITT-1, xenografts demonstrated both reduced tumor volume and mass after treatment with Lipclod, GW2580, and AZD7507. Furthermore, of the 8 SNU-1079 xenografts that were palpable at 3 weeks, only 4 from the GW2580 group and 6 from the AZD7507 group were large enough to recover at week 6, as they were no longer palpable and too small to detect. In the CC-LP-1 group, only 3 of the 8 tumors were detectable at 6 weeks. (In the WITT-1 line, 7 xenografts were recovered from the GW2580 and 8 from the AZD7507 group.) Depletion of macrophages using Lipclod, GW2580, or AZD7507 in all 3 xenografted lines resulted in a reduction in murine Wnt7b expression at the mRNA level[2].