BPR1R024 是一种选择性的集落刺激因子-1 受体(CSF1R) 抑制剂，具有口服活性。BPR1R024 具有有效的 CSF1R 抑制活性，IC₅₀ 值为 0.53 nM。BPR1R024 可用于免疫肿瘤学研究。

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-oncology.

Solid

IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB).

BPR1R024 (compound 12) has potent CSF1R inhibition activity with an IC50 value of 0.53 nM.
BPR1R024 exhibits weake AURA and AURB inhibitory activity in enzyme activity assay with IC50 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. has not independently confirmed the accuracy of these methods. They are for reference only.

BPR1R024 (compound 12) (oral; 100 mg/kg; twice a day) exhibits antitumor and immunomodulatory activity in a murine colon tumor model. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: R

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Powder -20°C 3 years；4°C 2 years

[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.