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Zosuquidar trihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Zosuquidar trihydrochloride图片
CAS NO:167465-36-3
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
唑喹达三盐酸盐
RS 33295-198 trihydrochloride
LY-335979 trihydrochloride
产品介绍
Zosuquidar (LY335979) trihydrochloride 是一种 P-糖蛋白 (P-gp) 抑制剂 (Ki=59 nM)。Zosuquidar trihydrochloride 具有抗肿瘤活性,并可用于急性骨髓性白血病 (AML) 的研究。
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.
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).
Clinical Trial
分子量

636.99

性状

Solid

Formula

C32H34Cl3F2N3O2

CAS 号

167465-36-3

中文名称

唑喹达三盐酸盐

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5699 mL7.8494 mL15.6988 mL
5 mM0.3140 mL1.5699 mL3.1398 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].