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CAS No.: 167354-41-8

Zosuquidar/唑喹达 Catalog No. CSN12903

Synonyms: RS 33295-198;LY-335979

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).

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实验方案

技术信息

生物活性

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 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^[4] (i.p.); 25 mg/kg - 80 mg/kg^[2] (p.o.); 20 mg/kg^[2] (i.v.)

给药途径
i.v., i.p., p.o.
临床研究

动物研究
剂量	Rat: 2 mg/kg - 20 mg/kg^[3] (i.v.) Mice: 25 mg/kg^[4] (i.p.); 25 mg/kg - 80 mg/kg^[2] (p.o.); 20 mg/kg^[2] (i.v.)
给药途径	i.v., i.p., p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00046930	-	-	Completed	-	-
NCT00046930	Leukemia Myel... more >>odysplastic Syndromes Collapse <<	Phase 3	Completed	-	-
NCT00129168	Leukemia, Myeloid	Phase 1 Phase 2	Completed	-	-

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参考文献

[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

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
- 1.8954 mL
- 9.4768 mL
- 18.9536 mL
- 5 mM
- 0.3791 mL
- 1.8954 mL
- 3.7907 mL
- 10 mM
- 0.1895 mL
- 0.9477 mL
- 1.8954 mL

技术信息

CAS号	167354-41-8	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C32H31F2N3O2	运输	蓝冰
分子量	527.60	别名	RS 33295-198;LY-335979

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