Zosuquidar (LY335979) 3HCl - 10mM in DMSO, high purity , CAS No.167465-36-3(DMSO)

Item Number

Z408366

• Specifications & Purity: 10mM in DMSO
• Biochemical and Physiological Mechanisms: Zosuquidar 3HCl (LY335979, RS 33295-198, D06387) is a potent modulator of P-glycoprotein-mediated multi-drug resistance with K_i of 60 nM in a cell-free assay. Phase 3.
• Storage Temp: Store at -80°C
• Shipped In: Ice chest + Ice pads

Product Description

Information

Zosuquidar (LY335979) 3HCl Zosuquidar 3HCl (LY335979, RS 33295-198, D06387) is a potent modulator of P-glycoprotein -mediated multi-drug resistance with K i of 60 nM in a cell-free assay. Phase 3.
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

Cell Data

cell lines：Murine mammary carcinoma cell line MDR EMT6/AR1.0

Concentrations：0.05 μM to 5 μM

Incubation Time：72 hours

Powder Purity:≥99%