Zosuquidar 3HCl
CAS No. | 167465-36-3 | Cat. No. | BCP02954 |
Name | Zosuquidar 3HCl | ||
Synonyms | LY335979;RS 33295-198; Zosuquidar trihydrochloride;LY335979;LY-335979; | ||
Formula | C32H31F2N3O2.3HCl | M. Wt | 636.99 |
Description | 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. | ||
Pathways | Neuro Signaling Pathway | ||
Targets | P glycoprotein |
Structure
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