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DDO-5936

Names

[ CAS No. ]:
2355377-13-6

[ Name ]:
DDO-5936

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

Biological Activity

[Description]:

DDO-5936 is a potent and specific Hsp90-Cdc37 PPI inhibitor. DDO-5936 can be used for the research of colorectal cancer[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> HSP
Signaling Pathways >> Cell Cycle/DNA Damage >> HSP

[Target]

Hsp90-Cdc37 PPI[1]


[In Vitro]

DDO-5936 is a Hsp90-Cdc37 PPI inhibitor with potency and specificity through binding to a critical site on Hsp90 involving Glu47[1].

[In Vivo]

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]. Animal Model: Mice[1] Dosage: 0~80 mg/kg Administration: P.o. Result: Showed a moderate effect at the high dose group.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C25H29N5O4S

[ Molecular Weight ]:
495.59

[ Storage condition ]:
-20°C


Related Compounds