BPR1R024-mesylate-DataSheet-生命科学试剂-MCE.pdf

Hotline: 400-820-3792 Inhibitors • Screening Libraries • Proteins www.MedChemE BPR1R024 mesylate Cat. No.: HY-132935A CAS No.: 2763365-40-6 分⼦式: C₂₅H₂₅F₃N₆O₅S 分⼦量: 578.56 作⽤靶点: c-Fms 作⽤通路: Protein Tyrosine Kinase/RTK 储存⽅式: Please store the product under the recommended conditions in the Certificate of Analysis. BIOLOGICAL ACTIVITY ⽣物活性 BPR1R024 mesylate 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 mesylate 是 BPR1R024 (HY-132935) 的等效物。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。 IC50 Target IC50: 0.53 nM (CSF1R); 10 μM (AURA); 1.40 μM (AURB) [1]. 体外研究 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: RAW264.7 and THP-1 cells