OARV-771 is a VHL-based BET degrader (PROTAC) with improved cell permeability. OARV-771 shows DC 50 s of 6, 1, and 4 nM for Brd4, Brd2 and Brd3, respectively.
性状
Solid
IC50 & Target[1][2]
BRD4 6 nM (DC50) BRD2 1 nM (DC50
体外研究(In Vitro)
OARV-771 shows antiproliferative effect with an EC50 value of 4 nM in MV4;11. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Klein VG, et al. Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. J Med Chem. 2021;64(24):18082-18101.
溶解度数据
In Vitro: DMSO : 100 mg/mL (101.25 mM; Need ultrasonic)配制储备液