Glycine, N-[4-[[2-(1-pyrrolidinyl)-4-pyrimidinyl]amino]phenyl]-N-[(2,4,6-trimethylphenyl)sulfonyl]-

Biological Activity

DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer[1]. DDO-5936 is a Hsp90-Cdc37 PPI inhibitor with potency and specificity through binding to a critical site on Hsp90 involving Glu47[1]. DDO-5936 (0~80 mg/kg; p.o.) shows effect at the high dose group[1].DDO-5936 is well tolerated for the absence of serious weight loss. DDO-5936 high dose groups show that tumor cells in the xenografts decreased significantly. DDO-5936 shows limited oral efficiency[1].

References

[1]. Wang L, et al. Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer. J Med Chem. 2020;63(3):1281-1297.