| 生物活性 | Zosuquidar (LY335979) trihydrochloride is aP-glycoprotein(P-gp) inhibitor (Ki=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research[1][2][3]. |
| IC50& Target | Ki: 59nM (P-glycoprotein)[1]. |
体外研究
(In Vitro) | Zosuquidar (0.3 μM; 48 h) enhances the cytotoxicity of DNR (substrates for P-glycoproteins) in P-glycoproteins active cell lines[2].
Zosuquidar (5-16 μM; 72 h) treatment alone shows high cytotoxic concentration to drug-sensitive and MDR cell lines[1].
Cell Cytotoxicity Assay[2] | Cell Line: | K562 and HL60 cells | | Concentration: | 0.3 μM | | Incubation Time: | 48 hours | | Result: | Enhanced the cytotoxicity of DNR (substrates for P-glycoproteins) in K562/DOX cells more than 45.5-fold. |
Cell Cytotoxicity Assay[1] | Cell Line: | CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells | | Concentration: | 5-16 μM | | Incubation Time: | 72 hours | | Result: | Showed IC50s of 6, 7, 15, 8, 7, 15, 11, 16, >5, >5 μM for CCRF-CEM, CEM/VLB100, P388, P388/ADR, MCF7, MCF7/ADR, 2780, 2780AD, UCLA-P3, UCLA-P3.003VLB cells, respectively. |
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体内研究
(In Vivo) | Zosuquidar (intraperitoneal injection; 30, 10, 3, or 1 mg/kg; once daily; 5 d) treatment shows a significant increase in life span[1].
Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin[1].
| Animal Model: | Mice implanted with P388/ADR tumors[1] | | 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[1] | | 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). |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
| 溶解性数据 | In Vitro: H2O : 5 mg/mL(7.85 mM;Need ultrasonic) DMSO : 1 mg/mL(1.57 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.5699 mL | 7.8494 mL | 15.6988 mL | | 5 mM | 0.3140 mL | 1.5699 mL | 3.1398 mL | | 10 mM | --- | --- | --- |
*请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。 In Vivo: 1. Zosuquidar is dissolved in 20% ethanol-saline[5].
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