SR-4835 (C09-1044-479)

InformationSR-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.TargetsCDK13 (Cell-free assay); CDK12 (Cell-free assay); CDK12 (Cell-free assay) 4.9 nM; 98 nM(Kd); 99 nMIn vitroSR-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 vivoSR-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. Specification: 0.98 Molecular Formula: C21H2OCl2N10O Molecular Weight: 499.36 PubChem CID: 139600338 Isomeric SMILES: CN1C=C(C=N1)N2C=NC3=C(N=C(N=C32)N4CCOCC4)NCC5=NC6=CC(=C(C=C6N5)Cl)Cl Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/S414251-SCI_567fd0e76560978bc0c64aa16b547aa0.pdf