Animal experiment:

Mice[1]Female SCID mice bearing RS4;11 xenograft tumors were dosed with a single intravenous dose of QCA570 (compound 35) at 5 mg/kg[1].

QCA570 is a potent BET degrader based on PROTAC, with an IC50 of 10 nM for BRD4 BD1 Protein.

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[1].

[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 Aug 9;61(15):6685-6704.