SR-4835 是有效，高选择性和 ATP 竞争性的 CDK12/CDK13 双重抑制剂。 SR-4835 与破坏 DNA 的化学疗法和 PARP 抑制剂协同作用，并引起三阴性乳腺癌 (TNBC) 细胞凋亡。 Information SR-4835 SR-4835 is a highly selective dual inhibitor of CDK12 and CDK13 with IC50 of 99 nM and Kd of 98 nM for CDK12 and IC50 of 4.9 nM for CDK13. SR-4835 disables triple-negative breast cancer (TNBC) cells. SR-4835 promotes synergy with DNA-damaging chemotherapy and PARP inhibitors. Targets CDK13 (Cell-free assay); CDK12 (Cell-free assay); CDK12 (Cell-free assay) 4.9 nM; 98 nM(Kd); 99 nM In vitro SR-4835 is a selective, potent dual inhibitor of CDK12 and CDK13, suppressing expression of DDR proteins. CDK12/CDK13 inhibition synergizes with DNA-damaging agents or PARP inhibition to trigger TNBC cell death. In vivo SR-4835 has potent in vivo anti-TNBC activity and augments the anti-cancer activity of cisplatin, irinotecan, and olaparib, which are standard-of-care therapeutics for TNBC. SR-4835 is well tolerated in mice after long-term dosing. SR-4835 cooperates with DNA-damaging chemotherapeutics. Cell Research(from reference) Cell lines：Human: MDA-MB-231, MDA-MB-436, HS578T, MDA-MB-468, FHC Concentrations：10-90 nM, 0.4-10 μM Incubation Time：4 h, 6 h, 72 h