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2413849-81-5

2413849-81-5 Structure

2413849-81-5 Structure
IdentificationBack Directory
[Name]

CAY10747
[CAS]

2413849-81-5
[Synonyms]

CAY10747
[Molecular Formula]

C42H48FNO6
[MOL File]

2413849-81-5.mol
[Molecular Weight]

681.85
Chemical PropertiesBack Directory
[Boiling point ]

816.3±65.0 °C(Predicted)
[density ]

1.24±0.1 g/cm3(Predicted)
[storage temp. ]

-20°C
[solubility ]

DMF: 30 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml
[form ]

A crystalline solid
[pka]

8.60±0.70(Predicted)
Hazard InformationBack Directory
[Uses]

Hsp90-Cdc37-IN-2 (Compound 41) is an inhibitor for the interaction between heat shock protein 90 (Hsp90) and cyclin 37 (Cdc37). Hsp90-Cdc37-IN-2 inhibits the proliferation of cancer cell A549, MCF-7, HOS and HepG2 with IC50 of 0.41-0.94 μM. Hsp90-Cdc37-IN-2 decreases the mitochondrial membrane potential, induces apoptosis, and arrest cell cycle at G0/G1 phase in A549[1].
[Biological Activity]

CAY10747 is an inhibitor of the protein-protein interaction between heat shock protein 90 (Hsp90) and cell division cycle 37 (Cdc37) and a derivative of celastrol .1 It decreases protein levels of the Hsp90-Cdc37 complex and the Hsp90-Cdc37 clients phosphorylated Akt and Cdk4 in A549 cells when used at a concentration of 5 μM. CAY10747 inhibits proliferation of A549, MCF-7, HOS, and HepG2 cells (IC50s = 0.41, 0.64, 0.9, and 0.94 μM, respectively) and induces apoptosis in A549 cells.
[References]

1.Li, N., Xu, M., Wang, B., et al.Discovery of novel celastrol derivatives as Hsp90-Cdc37 interaction disruptors with antitumor activityJ. Med. Chem.62(23)10798-10815(2019)
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