产品描述:
DDO-5936 is an inhibitor of the protein-protein interaction between heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37).{66818} It inhibits the Hsp90-Cdc37 interaction in HCT116 human colorectal cancer cells when used at concentrations of 5, 10, and 25 µM. DDO-5936 is selective for inhibition of the Hsp90-Cdc37 interaction over inhibition of 20 kinases (IC50s = >100 µM for all) and inhibits the proliferation of HCT116 cells (IC50 = 8.99 µM). It also reduces the levels of the Hsp90 kinase client Cdk4 and induces cell cycle arrest at the G0/G1 phase in a Cdc37-dependent manner in HCT116 cells when used at concentrations of 10 and 25 µM. DDO-5936 (50 and 100 mg/kg per day) reduces tumor growth and tumor weight in an HCT116 mouse xenograft model.