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

CAS: 167465-36-3 Cat. No.: Z408366 Molecular Weight: 637 EC Number: 808-502-9 PubChem CID: 153997

GRADE & PURITY 10mM in DMSO

Synonyms

RS 33295-198 (D06387) 3HCl | 1-Piperazineethanol, 4-[(1aα,6α,10bα)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-,trihydrochloride

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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%

Specifications

Synonyms

RS 33295-198 (D06387) 3HCl | 1-Piperazineethanol, 4-[(1aα, 6α, 10bα)-1, 1-difluoro-1, 1a, 6, 10b-tetrahydrodibenzo[a, e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-, trihydrochloride

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

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Names and Identifiers

• Isomeric SMILES: C1CN(CCN1C[C@H](COC2=CC=CC3=C2C=CC=N3)O)C4C5=CC=CC=C5[C@H]6[C@H](C6(F)F)C7=CC=CC=C47.Cl.Cl.Cl
• Alternate CAS: 167354-41-8
• PubChem CID: 153997
• Molecular Weight: 637