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编 号:F200524
分子式:C32H34Cl3F2N3O2
分子量:636.99
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5mg
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10mg
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50mg
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100mg
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生物活性:
Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.

体内研究:
Zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) treatment shows a significant increase in life span.?Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin.Animal Model:Mice implanted with P388/ADR tumors
Dosage:30, 10, 3, or 1 mg/kg
Administration:Intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 days
Result:Exihibited a significantly increased survival compared to the group treated with Doxorubicin alone (P<0.001).
Animal Model:Mice implanted with P388 or P388/ADR murine leukemia cells
Dosage:30 mg/kg
Administration:Intraperitoneal injection; 30 mg/kg; once daily; 5 days
Result:Observed significant antitumor activity against the MDR P388/ADR cell lines when mice were treated with a combined dose of 30 mg/kg LY335979 and 1 mg/kg Doxorubicin (P=0.1).

体外研究:
Zosuquidar (0.3 μM; 48 h) enhances the cytotoxicity of DNR (substrates for P-glycoproteins) in P-glycoproteins active cell lines.?Zosuquidar (5-16 μM; 72 h) treatment alone shows high cytotoxic concentration to drug-sensitive and MDR cell lines.
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