Cayman SR 4835

SR 4835 is an inhibitor of cyclin-dependent kinase 12 (Cdk12) and Cdk13.¹ It binds to Cdk12 and Cdk13 (K_ds = 98 and 4.9 nM, respectively) and inhibits Cdk12- and Cdk13-dependent phosphorylation of RNA polymerase II in MDA-MB-231 cells (EC₅₀ = 105.5 nM). SR 4835 inhibits the proliferation of MDA-MB-231, MDA-MB-468, Hs 578T, and MDA-MB-436 breast cancer cells (EC₅₀s = 15.5, 22.1, 19.9, and 24.9 nM, respectively). It induces the DNA damage response and apoptosis in MDA-MB-231 cells when used at concentrations ranging from 30 to 90 nM. In vivo, SR 4835 (20 mg/kg) reduces tumor volume and decreases the number of mice with tumors greater than 1,000 mm³ in a patient-derived xenograft (PDX) model of breast cancer.

WARNING This product is not for human or veterinary use.