PROTAC AR-V7 degrader-1 (Compound 6) is a potent, orally bioavailable and selective AR-V7 degrader with the DC 50 of 0.32 μM by recruiting VHL E3 ligase to Androgen receptor (AR) DNA binding domain (DBD) binder. PROTAC AR-V7 degrader-1 exhibits activity against 22Rv1 cell-line expressing AR-V7 with the EC 50 of 0.88 μM.
性状
Solid
IC50 & Target[1][2]
VHL
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Archana Bhumireddy, et al. Design, synthesis, and biological evaluation of phenyl thiazole-based AR-V7 degraders. Bioorg Med Chem Lett. 2022 Jan 1;55:128448.
溶解度数据
In Vitro: DMSO : 110 mg/mL (139.41 mM; Need ultrasonic)配制储备液