| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| Z408366-1ml | 1ml | Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience! | $393.90 |
P-gp Modulators
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Storage Temp | Store at -80°C |
| Shipped In | Dry ice |
| 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. 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 lines：Murine mammary carcinoma cell line MDR EMT6/AR1.0 Concentrations：0.05 μM to 5 μM Incubation Time：72 hours Powder Purity:≥99% |
| Canonical SMILES | Cl.Cl.Cl.OC(COC1=CC=CC2=C1C=CC=N2)CN3CCN(CC3)C4C5=C(C=CC=C5)C6C(C7=C4C=CC=C7)C6(F)F |
|---|---|
| Molecular Weight | 636.99 |
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