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编 号:F287147
分子式:C16H11N3O3
分子量:293.28
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1mg
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5mg
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10mg
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生物活性:
Alsterpaullone (9-Nitropaullone) is a potent CDK inhibitor, with IC50s of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also competes with ATP for binding to GSK-3alpha/GSK-3beta with IC50s of both 4 nM. Alsterpaullone has antitumor activity, and possesses potential for the study in neurodegenerative and proliferative disorders. Alsterpaullone induces apoptosis in leukemia cell line.

体内研究:
Alsterpaullone (30 mg/kg, s.c., daily for 2 weeks) reduces tumor growth and increases survival in medulloblastoma xenografts.Animal Model:5-6 week old athymic nude mice
Dosage:30 mg/kg
Administration:Subcutaneous injections, daily for 2 weeks
Result:Antitumor effect in Group 3 medulloblastomas.

体外研究:
Alsterpaullone (0.3, 1, 3 μM; 8 hours) induces apoptosis in leukemia cell line.Alsterpaullone (5, 10, 15, 20, 25, 30 μM; 48 and 72 hours) inhibits the growth of HeLa cells in dose-and time-dependent manner. Treatment with Alsterpaullone causes a time-dependent inhibition of cell growth too. Alsterpaullone (20?μM) induces cell death depending on caspase activity.
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