PROTAC AR-V7 degrader-2

PROTAC AR-V7 degrader-2 is an AR-based PROTAC. PROTAC AR-V7 degrader-2 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. PROTAC AR-V7 degrader-2 induces apoptosis[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> PROTAC >> PROTAC

Signaling Pathways >> Others >> Androgen Receptor

PROTAC AR-V7 degrader-2 (compound 16; 0-20 μM; 4 d; 22Rvl 细胞) 以剂量依赖性方式抑制细胞生长[1]。 PROTAC AR-V7 degrader-2 (10 μM; 4 d; 22Rvl 细胞) 降低 AR-V7 蛋白水平[1]。 PROTAC AR-V7 degrader-2 (1 μM; 0-48 h; 22Rvl 细胞) 诱导细胞凋亡并增加膜联蛋白-V 染色[1]。 Cell Viability Assay[1] Cell Line: 22Rvl cells Concentration: 0-20 μM Incubation Time: 4 days Result: Reduced the cell count by less than 50 percent. Apoptosis Analysis[1] Cell Line: 22Rvl cells Concentration: 1 μM Incubation Time: 0-48 h Result: Induced cell apoptosis in 22Rvl cells. Western Blot Analysis[1] Cell Line: 22Rvl cells Concentration: 10 μM Incubation Time: 4 days Result: Reduced AR-V7 protein levels.

PROTAC AR-V7 degrader-2 (compound 16; 2.5 mg/mL; 瘤内注射) 抑制带有 22Rvl-EnzR 肿瘤异种移植物的 nu/nu 小鼠的肿瘤生长[1]。 Animal Model: nu/nu mice with 22Rvl-EnzR tumor xenografts[1] Dosage: 2.5 mg/mL Administration: intratumor injection Result: Inhibited tumor growth in nu/nu mice with 22Rvl-EnzR tumor xenografts.

[1]. Jenny D, et, al. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor. WO2021236695.