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编 号:F176778
分子式:C36H47N5O4
分子量:613.79
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生物活性:
Indinavir (MK-639 free base) is an orally active and selective HIV-1 protease inhibitor with a Ki of 0.54 nM for PR. Indinavir exhibits anticancer activity by inhibiting the activation of MMPs-2 hydrolysis, anti-angiogenesis and inducing apoptosis. Indinavir is also a SARS-CoV 3CLpro inhibitor.

体内研究:
Indinavir (70 mg/kg; i.g.; once a day for 3 weeks) inhibits the growth of hepatocarcinoma cells in vivo.Animal Model:Nude mice(s.c. into Huh7 and SK-HEP-1 cells).
Dosage:70 mg/kg
Administration:Oral gavage; once a day for 3 weeks.
Result:Delaied the growth of s.c. implanted hepatocarcinoma xenografts in nude mice compared with placebo.

体外研究:
Indinavir (0-50 μM; 18 h) blocks lymphocyte cell cycle in G0/G1 phase in PBMCs cells and impairs lymphoproliferative responses.Indinavir (40 μM-40 nM; 5 days) inhibits cell invasion and (40 μM-40 nM; 48 h) MMPs-2 activation of the Huh7 and SK-HEP-1 hepatocarcinoma cells in vitro.
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