Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 2 mg | In stock | $ 102 | |
| 4 mg | In stock | $ 193 | |
| 8 mg | In stock | $ 274 | |
| 20 mg | In stock | $ 578 | |
| 40 mg | In stock | $ 890 |
| Description | Zosuquidar (LY335979) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM. Phase 3. |
| Targets&IC50 | P-gp:60 nM(Ki) |
| In vitro | LY335979 competitively inhibits equilibrium binding of [3H]vinblastine to Pgp by blocking [3H]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. |
| In vivo | Zosuquidar trihydrochloride is only moderately active as an inhibitor of P-gp at the blood-brain. An oral dose of 25 mg/kg of zosuquidar trihydrochloride increases the brain concentrations by about 2.5-fold at 1 h and 5-fold at 24 h after paclitaxel administrationbarrier. Zosuquidar enhances the brain uptake of nelfinavir in a dose-dependent manner. Brain tissue/plasma nelfinavir concentration ratios increase from 0.06±0.03 in the absence of zosuquidar administration and 0.09±0.02 between 2 and 6 h after a 2 mg/kg intravenous dose of zosuquidar to 0.85±0.19 after 6h and 1.58±0.67 after 20 mg/kg zosuquidar. |
| Synonyms | RS 33295-198 (D06387) 3HCl, Zosuquidar (LY335979) 3HCl, LY-335979 trihydrochloride, RS 33295-198 trihydrochloride, Zosuquidar 3HCl |
| CAS No. | 167465-36-3 |
| Chemical Formula | C32H34Cl3F2N3O2 |
| Molecular Weight | 636.99 |
| Solubility | DMSO: 31.9 mg/mL (50 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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