Zosuquidar trihydrochloride 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride|cas:167465-36-3|西域试剂

Zosuquidar trihydrochloride 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride,99.79%

产品编号：Bellancom-50671| CAS NO：167465-36-3| 分子式：C₃₂H₃₄Cl₃F₂N₃O₂| 分子量：636.99

Zosuquidar trihydrochloride是P-糖蛋白的抑制剂， Ki值为59 nM。

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货号	价格	库存与货期
Bellancom-50671	￥1050.00	杭州北京（现货）
Bellancom-50671	￥1600.00	杭州北京（现货）
Bellancom-50671	￥5700.00	杭州北京（现货）
Bellancom-50671	￥9500.00	杭州北京（现货）

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Zosuquidar trihydrochloride 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 (K_i=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 a P-glycoprotein (P-gp) inhibitor (K_i=59 nM). Zosuquidar trihydrochloride shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay

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

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.
Zosuquidar (intraperitoneal injection; 30 mg/kg; once daily; 5 d) treatment shows the potentiation with a combined of Doxorubicin.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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).

性状

Solid

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 mg	5 mg	10 mg

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].

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。

参考文献

. A H Dantzig, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9. [Content Brief]

. Ruoping Tang, et al. Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML). BMC Cancer. 2008 Feb 13;8:51. [Content Brief]

. Larry D Cripe, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood [Content Brief]

化学品安全说明书(MSDS)

下载MSDS

质检证书(COA)

产品编号(Item Number)

批号(Lot Number)

1. 物质的识别

产品名：	LY335979 trihydrochloride
CAS号：	167465-36-3
制造商/供应商：	西域试剂网站：www.hzbp.cn 邮件：13911702513@139.com

2. 合成/成分数据

产品名：	LY335979 trihydrochloride
别名：	Zosuquidar trihydrochloride
分子式：	C32H31F2N3O2.3HCl
分子量：	637.00

3. 急救措施

吸入后：	如果吸入，移至空气新鲜处，如果呼吸困难，给输氧，如呼吸停止，给予人工呼吸。
皮肤接触后：	用大量的水冲洗，移除污染的衣服和鞋子。
眼睛接触后：	检查并取下隐形眼镜，并用大量的水冲洗；呼叫医生。
吞食后：	如果吞食，用大量纯净水漱口；呼叫医生。

4. 消防措施

适当的灭火剂：	雾状水，二氧化碳，干粉或泡沫。
防护设备：	穿戴自给式呼吸器和防护服，以防止与皮肤和眼睛接触。

5. 泄漏应急处理

安全防范措施：	封锁泄漏区域；穿戴自给式呼吸器，防护服和厚橡胶手套。
清洁/收集措施：	使用液体粘合原料（硅藻土，通用粘合剂）吸取精细粉末；使用酒精擦洗表面和设备除去污渍；根据第11条处理被污染的材料。

6. 处理和储存

安全处理说明：	避免吸入和接触皮肤，眼睛及衣物；材料可能略微具有刺激性。
储存：	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月

7. 接触控制和个人防护

呼吸设备：	NIOSH / MSHA认可的呼吸器。
双手保护：	耐化学腐蚀的橡胶手套。
眼睛防护：	化学安全护目镜。

8. 稳定性和反应活性

稳定性：	按照说明存储是稳定的；避免强氧化剂。
热分解/其他要避免的情况：	避免光和热。

9. 毒性资料

急性毒性：	无可用资料。
主要刺激性影响：	无可用资料。
在皮肤上：	无可用资料。
对眼睛：	无可用资料；可能具有刺激性。

10. 生态资料

一般注意事项：

无可用资料。

11. 废弃处置

按照所在国家，省份，县市和地方的法规处置。

12. 运输信息

正确的运输名称：	无
非危险品运输：	这种物质被视为非危险品运输。

13. 法规信息

尚未有针对此产品作出的化学安全性评估。

14. 其他信息

[1]. Cripe LD, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood.?201

[2]. Tang R, et al. Zosuquidar?restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AmL). BMC Cancer.?2008 Feb 13;8:51.?

[3]. Kemper EM, et al. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol. 2004 Feb;53(2):173-8.

[4]. Anderson BD, et al. Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats. Drug Metab Dispos. 2006 Apr;34(4):653-9.

[5]. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson's disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9.

Zosuquidar trihydrochloride 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride,99.79%

Zosuquidar trihydrochloride 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride

化学品安全说明书(MSDS)

质检证书(COA)

1. 物质的识别

2. 合成/成分数据

3. 急救措施

4. 消防措施

5. 泄漏应急处理

6. 处理和储存

7. 接触控制和个人防护

8. 稳定性和反应活性

9. 毒性资料

10. 生态资料

11. 废弃处置

12. 运输信息

13. 法规信息

14. 其他信息

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