BPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC50 value of 0.53 nM[1].
BPR1R024 exhibits weake AURA and AURB inhibitory activity in enzyme activity assay with IC50 values of 锛?0 渭M and 1.40 渭M, respeactively[1].
BPR1R024 (0-500 nM) significantly suppressed the CSF1R signal in a dose-dependent manner[1].
BPR1R024 (10 nM, 100 nM) inhibits CSF1/CSF1R signaling-mediated TNF-伪 production[1].
BPR1R024 (0-10 渭M) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth[1].
BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model[1].
[1]. Lee KH, et al. Discovery of BPR1R024, an Orally Active and Selective CSF1R Inhibitor that Exhibits Antitumor and Immunomodulatory Activity in a Murine Colon Tumor Model. J Med Chem. 2021 Oct 14;64(19):14477-14497.