唑喹达三盐酸盐
| CAS号 | 167465-36-3 | 货号 | BCP02954 |
| 中文名 | 唑喹达三盐酸盐 | ||
| 英文名 | Zosuquidar 3HCl | ||
| 中文别名 | |||
| 英文别名 | LY335979;RS 33295-198; Zosuquidar trihydrochloride;LY335979;LY-335979; | ||
| 分子式 | C32H31F2N3O2.3HCl | 分子量 | 636.99 |
| 生物活性 | LY335979 competitively inhibits equilibrium binding of vinblastine to Pgp by blocking azidopine photoaffinity labeling of the Pgp in CEM/VLB100 plasma membranes.LY335979 alone shows the cytotoxicity to drug-sensitive and MDR cell lines with IC50 ranging from 6 μM-16 μM and produces its ability to completely reverse the resistance of the oncolytics (vinblastine, doxorubicin, or etoposide) to the MDR cell lines P388/ADR, MCF7/ADR, 2780AD, or UCLA-P3.003VLB at concentration of 0.1 and 0.5 μM. LY335979 significantly restores drug sensitivity in P-gp-expressing leukemia cell lines including K562/HHT40, K562/HHT90, K562/DOX and HL60/DNR, and enhances the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AML blasts with active P-gp. A latest paper indicates that LY335979 completely inhibits apically directed transport of (Z)-endoxifen in the ABCB1-transduced cells. | ||
| 信号通路 | Neuro Signaling Pathway | ||
| 靶 点 | P glycoprotein | ||
结构式
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