QCA570 is a PROTAC connected by ligands for Cereblon and BET, with an IC 50 of 10 nM for BRD4 BD1 Protein.
性状
Solid
IC50 & Target[1][2]
BRD4 BD1 10 nM (IC50)
体外研究(In Vitro)
QCA570 is an extremely potent and highly efficacious BET degrader, capable of degrading BET proteins at low picomolar (pM) concentrations in leukemia cells. QCA570 inhibits cell growth in MV4;11, MOLM-13, and RS4;11 cell lines with IC50 values of 8.3, 62, and 32 pM, respectively. QCA570 is the most potent and efficacious BET degrader reported to date. 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, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Qin C, et al. Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression. J Med Chem. 2018 A
溶解度数据
In Vitro: DMSO : 40 mg/mL (57.49 mM; Need ultrasonic)配制储备液