Bioactivity | BPR1R024 is an orally active and selective colony-stimulating factor-1 receptor (CSF1R) inhibitor. BPR1R024 has potent CSF1R inhibition activity with an IC50 value of 0.53 nM. BPR1R024 can be used for the research of immuno-oncology[1]. | ||||||||||||
Target | IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB). | ||||||||||||
Invitro | 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 >10 μM and 1.40 μM, 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-α production[1].BPR1R024 (0-10 μM) specifically inhibits protumor M2-like macrophage survival with a minimal effect on antitumor M1-like macrophage growth[1]. Western Blot Analysis[1] Cell Line: | ||||||||||||
In Vivo | BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model[1]. Animal Model: | ||||||||||||
Name | BPR1R024 | ||||||||||||
CAS | 2503015-75-4 | ||||||||||||
Formula | C24H21F3N6O2 | ||||||||||||
Molar Mass | 482.46 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |