QCA570

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

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

Signaling Pathways >> PROTAC >> PROTAC

Research Areas >> Cancer

BRD4 BD1:10 nM (IC50)

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].

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].

[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.

(+)-JQ1 | GSK126 | Tazemetostat (EPZ-6438) | Birabresib (OTX015) | A 485 | Curcumin | ARV-771 | ARV-825 | I-BET762 | BI 2536 | GSK343 | C646 | 3-Deazaneplanocin A (hydrochloride) | I-BET151 | 666-15