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编 号:F242841
分子式:C23H24O8
分子量:428.43
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10mM*1mL in DMSO
792
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1mg
274
In-stock
5mg
720
In-stock
10mg
1200
In-stock
50mg
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In-stock
100mg
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In-stock
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生物活性:
Wortmannin (SL-2052; KY-12420) is a potent, selective and irreversible PI3K inhibitor with an IC50 of 3 nM. Wortmannin also blocks autophagy formation, and potently inhibits Polo-like kinase 1 (PlK1) and Plk3 with IC50s of 5.8 and 48 nM, respectively.

体内研究:
Wortmannin (oral gavage; daily; in Scid mice; one group of eight mice is dosed with Wortmannin 1 mg/kg for all 14 days. The second group of eight mice is dosed with Wortmannin 1.5 mg/kg for the first 5 days and the dose is decreased to 1 mg/kg for the remaining treatment period) treatment significantly slower the growth rate of murine C3H mammary tumor and human MCF-7 breast cancer xenograft. A dose of 1 mg/kg Wortmannin for 7 days decrease the tumor burdens in mice with established murine C3H mammary tumors by 54% relative to controls. Human MCF-7 breast cancer xenograft burdens are decreased by 97% relative to controls after 14 days of 1 mg/kg Wortmannin beginning 1 day after tumor implantation.Animal Model:Scid mice with the murine C3H mammary tumor or human MCF-7 breast cancer xenograft
Dosage:1 mg/kg and 1.5 mg/kg
Administration:Oral gavage; daily; one group 1 mg/kg for 14 days; second group 1.5 mg/kg for 5 days then 1.0 mg/kg for 9 days.
Result:The growth rate of the treated tumors was significantly slower during drug administration than that of nontreated tumors.

体外研究:
Wortmannin (0-100 nM; 24-72 hours) inhibits the proliferation of K562 cells in a time- and dose-dependent manner. The IC50 values at 24 hour, 48 hour, and 72 hour are 25±0.10 nM, 12.5±0.08 nM, and 6.25±0.11 nM, respectively.Wortmannin prevents nuclear entry of YAP.
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