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CAS No.: 167465-36-3

Zosuquidar 3HCl/唑喹达三盐酸盐 Catalog No. CSN12751

Synonyms: RS 33295-198 trihydrochloride;LY-335979 trihydrochloride;LY-335979 3HCl

Zosuquidar 3HCl is the 3HCl form of Zosuquidar. Zosuquidar is P-gp modulator that inhibited Pgp-ATPase activity 50-60% at 2 and 10μM and had no effect at 0.08 and 0.4μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 P-gp

Ki:60nM
描述The multidrug resistance is an obstacle in the chemotherapy treatment (such as doxorubicin, vincristine, paclitaxel, TKIs) for many solid and haematological tumours. Many factors can cause the multidrug resistance. Among them, the overexpression of P-gp (ABCB1), an ATP-binding cassette (ABC) drug efflux transporter, on the surface of resistant cells is considered as a key factor mediating multidrug resistance. Zosuquidar Trihydrochloride is the trihydrochloride form of Zosuquidar. Zosuquidar is P-gp modulator that inhibited Pgp-ATPase activity 50-60% at 2 and 10μM and had no effect at 0.08 and 0.4μM (measured by P-gp ATPase activity). However, the modulator activity of Zosuquidar is not dependent on inhibition of the ATPase activity associated with P-gp. Zosuquidar works both in vitro and in vivo. Combined treatment with Zosuquidar at 0.1μM could fully restored sensitivity of CEM/VLB₁₀₀ cells to vinblastine, doxorubicin, etoposide and Taxol, and showed a prolonged effect up to 24h at concentration of 0.5μM in cytotoxicity assay of doxorubicin. The effect of Zosuquidar on restoring sensitivity of different compound may due to its blocking the affinity of compound to cell plasma membranes P-gp and competitively inhibited equilibrium binding of compound to P-gp (Ki=~60nM). Co-administration of Zosuquidar (20mg/kg, i.v.) with doxorubicin or etoposide significantly increased the life span of mice bearing P388/ADR murine leukemia cells, compared with group treated with agent alone. Also Zosuquidar (30mg/kg) enhanced the antitumor activity of Taxol in a multidrug-resistant human non-small cell lung carcinoma nude mouse xenograft model. However this in vivo increased life span achieved by Zosuquidar was lack of effect on pharmacokinetics^[1].

动物研究

剂量

Rat: 2 mg/kg - 20 mg/kg^[3] (i.v.); Mice: 25 mg/kg, 80 mg/kg^[2] (p.o.)

给药途径

i.v., p.o.

动物药代数据

Animal	Mice^[2]
Dose	20 mg/kg
Administration	i.v.
V_d	9.9 L/kg
T_1/2β	2.1 h
CL	3.3 l/h/kg
T_1/2α	15 min
AUC_0→8h	5960 ± 240 ng·h/ml

临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT00046930 Leukemia Myel... more >>odysplastic Syndromes Collapse << Phase 3 Completed - -
NCT00046930 - - Completed - -
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00046930	Leukemia Myel... more >>odysplastic Syndromes Collapse <<	Phase 3	Completed	-	-
NCT00046930	-	-	Completed	-	-

[1] Dantzig AH, Shepard RL, et al. Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 1996 Sep 15;56(18):4171-9.
[2] Kemper EM, Cleypool C, et al. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol. 2004;53(2):173-8.
[3] Anderson BD, May MJ, 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. Epub 2006 Jan 24.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.5699 mL
- 7.8495 mL
- 15.6989 mL
- 5 mM
- 0.3140 mL
- 1.5699 mL
- 3.1398 mL
- 10 mM
- 0.1570 mL
- 0.7849 mL
- 1.5699 mL

技术信息

CAS号

167465-36-3

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C32H34Cl3F2N3O2

运输

蓝冰

分子量

636.99

别名

RS 33295-198 trihydrochloride;LY-335979 trihydrochloride;LY-335979 3HCl;RS-33295198 3HCl;Zosuquidar (hydrochloride);RS 33295-198;LY-335979;D06387;Zosuquidar HCl;Zosuquidar 3HCl;唑喹达三盐酸盐

溶解度

DMSO	100.0 mg/mL (157.0 mM)
Water	22.0 mg/mL (34.5 mM)
Ethanol	Insoluble

动物实验配方

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Zosuquidar 3HCl/唑喹达三盐酸盐 Catalog No. CSN12751

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