产品
编 号:F751487
分子式:C35H44ClN3O6
分子量:638.19
产品类型
结构图
CAS No: 2361009-68-7
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产品详情
生物活性:
Hsp90-Cdc37-IN-3 (Compound 9) is a novel celastrol?imidazole derivative with anticancer activity. Hsp90-Cdc37-IN-3 inhibits Hsp90?Cdc37 by covalent-binding, and induces apoptosis.
体内研究:
Hsp90-Cdc37-IN-3 (Compound 9) (0-1 mg/kg; i.p.; once a day, 21 days) shows strong antitumor activity with no significant toxicity.Animal Model:Female BALB/c nude mice at 6 weeks old.
Dosage:0.5 mg/kg or 1 mg/kg. Mice were inoculated subcutaneously with A549 cells (1*107 in 100 μL of PBS for each mouse).
Administration:Intraperitoneal injection, once a day, 21 days
Result:Decreased tumor weight and enhanced TIR without show toxicity.
体外研究:
Hsp90-Cdc37-IN-3 (Compound 9) (24 h) shows broad-spectrum antitumor potential with IC50 values of 0.54, 0.59, 0.57, and 0.57 μM against A549, HTC116, U2OS, and MDA-MB231 cells, respectively.Hsp90-Cdc37-IN-3 (0-5 μM, 12 h) inhibits Hsp90?Cdc37 and influences the function of apoptosis-related proteins by covalently combining with both Hsp90 and Cdc37.Hsp90-Cdc37-IN-3 (0-0.8 μM, 48 h) induces apoptosis significantly in A549 cells.Hsp90-Cdc37-IN-3 (0-0.4 μM, 24 h) arrests the cell cycle in the G0/G1 phase in a dose-dependent manner.