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| 中文名: | 唑喹达三盐酸盐;唑喹达三盐酸盐 |
| 中文别名: | Zosuquidar 三盐酸盐;(2R)-1-{4-[(1aR,6r,10bS)-1,1-二氟-1,1a,6,10b-四氢二苯并[a,e]环丙并[c]环庚烯-6-基]哌嗪-1-基}-3-(喹啉-5-基氧基)丙-2-醇三盐酸盐 |
| 英文名称： | LY335979(Zosuquidar) |
| 英文别名： | RS 33295-198; Zosuquidar trihydrochloride;LY335979;LY-335979; (2R)-1-{4-[(1aR,6r,10bS)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]piperazin-1-yl}-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride;(2R)-Anti-5-[3-[4-(10,11-difluoromethanodibenzosuber-5-yl)piperazin-1-yl]-2-hydroxypropoxy]quinoline hydrochloride |
| CAS No.: | 167465-36-3 |
| 分子式: | C32H31F2N3O2.3HCl |
| 分子量: | 636.99 |
| 性状: | 属性溶解性Soluble in DMSO (100 mg/mL at 25 °C), water (23 mg/mL at 25 °C), ethanol (<1 mg/mL at 25 °C), and methanol.存贮条件储存温度-20°C描述产品介绍Zosuquidar (LY335979) 3HCl是一种有效的P-glycoprotein（P-糖蛋白）介导的多药耐抗性的调节剂，Ki为60 nM。Phase 3。用途A modulator of Pgp.生化机理Zosuquidar trihydrochloride is a potent modulator of P-glycoprotein-mediated(Mdr-1) multidrug resistance. This compound exhibits an IC50=60 nM. Zosuquidar trihydrochloride competitively inhibits equillibrium binding of drugs to Mdr-1 and shows an ability to reverse drug resistance to multiple oncolytics. |
| 储存: | 储存温度-20°C |
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| 用途: | LY335979(Zosuquidar) is a selective Pgp (P-glycoprotein) inhibitor with a Ki of 59 nM, and does not modulate MRP-mediated resistance by MRP1 (ABCC1) and MRP2 (ABCC2). LY335979 significantly enhanced the survival of mice implanted with Pgp-expressing murine leukemia (P388/ADR) when administered in combination with either daunorubicin, doxorubicin or etoposide. Coadministration of LY335979 with paclitaxel compared to paclitaxel alone significantly reduced the tumor mass of the Pgp-expressing UCLA-P3.003VLB lung carcinoma in a xenograph model. LY335979 was without significant effect on the pharmacokinetics of these anticancer agents. [1] |
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