Zosuquidar 3HCl

  • Chemical Properties
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
  • Biological Activity
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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