CSRM617-DataSheet-生命科学试剂-MedChemExpress.pdf免费

Hotline: 400-820-3792 Inhibitors • Agonists • Screening Libraries www.MedChemE CSRM617 Cat. No.: HY-122611 CAS No.: 787504-88-5 分⼦式: C₁₀H₁₃N₃O₅ 分⼦量: 255.23 作⽤靶点: Androgen Receptor; Apoptosis 作⽤通路: Others; Apoptosis 储存⽅式: Please store the product under the recommended conditions in the COA. BIOLOGICAL ACTIVITY ⽣物活性 CSRM617 是转录因⼦ ONECUT2 (OC2，雄激素受体 AR 的主要调节剂) 的选择性⼩分⼦抑制剂，在 SPR 测定中 Kd 为7.43 uM，直接与 OC2-HOX 结构域结合。CSRM617 通过切割 Caspase-3 和 PARP 诱导细胞凋亡 ( apoptosis)。CSRM617 在⼩⿏的前列腺癌模型中耐受性良好。 体外研究 CSRM617 (0.01-100 μM; 48 hours) inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells [1].CSRM617 (10-20 μM; 48 hours) induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion [1].CSRM617 (20 μM; 72 hours) induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP [1]. REFERENCES [1]. Rotinen M, et al. ONECUT2 is a targetable master regulator of lethal prostate cancer that suppresses the androgen axis. Nat Med. 2018 Dec;24(12):1887-1898. McePdfHeight Caution: Product has not been fully val