Description
BPR1R024 is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC 50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncologyIn VitroBPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC 50 value of 0.53 nM. BPR1R024 exhibits weake AURA and AURB inhibitory activity in enzyme activity assay with IC 50 values of ＞10 µM and 1.40 µM, respeactively. BPR1R024 (0-500 nM) significantly suppressed the CSF1R signal in a dose-dependent manner. BPR1R024 (10 nM, 100 nM) inhibits CSF1/CSF1R signaling-mediated TNF-α production. BPR1R024 (0-10 µM) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: RAW264.7 and THP-1 cells Concentration: 0-500 nM Incubation Time: 16 h Result: Significantly suppressed the CSF1R signal in a dose-dependent manner, at concentrations of approximately 50-75 and 1-10 nM in RAW264.7 and THP-1 cells, respectively.In VivoBPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Rats Dosage: 5, 20, 25 mg/kg Administration: IV, PO Result: Exhibited high systemic drug exposure with the dose-normalized area under curve (DNAUC) values of 3635 ng/mL*h by the IV route and 362 ng/mL*h by the PO route and the modification increased oral bioavailability (F=35%). Animal Model: C57BL/6 mice (six-week-old, male) Dosage: 100 mg/kg Administration: Oral, twice a day Result: Delayed the MC38 murine colon tumor growth and reversed the immunosuppressive tumor microenvironment with the increased M1/M2 ratio.Form:SolidIC50& Target:IC50: 0.53 nM (CSF1R),10 µM (AURA),1.40 µM (AURB)