Name: LY335979 (Zosuquidar 3HCL)
Price: 244.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    LY335979 is a selective inhibitor of P-Gp with IC50 value of 1.2 nM [1, 2].
    P-gp (P-glycoprotein) is a member of ATP-binding cassette (ABC) transporters and plays a pivotal role in pumping many foreign substances out of cells. It has been reported that abnormal expression of P-Gp is correlated with the multidrug resistance of tumor cells [3].
    LY335979 is a potent P-Gp inhibitor and has a different selectivity with the reported P-Gp inhibitor cyclosporin A or verapamil. In drug-resistant cell line HL60/VCR with highly expression of P-Gp, LY335979 exhibited highly restore ability of P-Gp than cyclosporin A or verapamil and the IC 50 value of 1.2 nM [1]. When tested with a panel of cell lines over-expressed P-Gp (CEM/VLB100, MCF-7/ADR, 2780AD, P388/ADR, and UCLA-P3.003VLB), administration of LY335979 reversed the cells resistance to Vinblastine, Doxorubicin, Btoposide and Taxol by inhibiting P-Gp activity [2].
    In female nude mice model with UCLA-P3.003VLB MDR tumor cells subcutaneous xenograft, pre-treated with LY335979 (30mg/kg) restored tumor cells sensitivity to Taxol (20 mg/kg) which combination markedly suppressed solid tumor growth compared with control group [2].
    
    1. Green, L.J., P. Marder, and C.A. Slapak, Modulation by LY335979 of P-glycoprotein function in multidrug-resistant cell lines and human natural killer cells. Biochem Pharmacol, 2001. 61(11): p. 1393-9.
    2. Dantzig, A.H., et al., Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res, 1996. 56(18): p. 4171-9.
    3. Hu, T., et al., Reversal of P-glycoprotein (P-gp) mediated multidrug resistance in colon cancer cells by cryptotanshinone and dihydrotanshinone of Salvia miltiorrhiza. Phytomedicine, 2014. 21(11): p. 1264-72.
- Properties
  - Alternative Name
    
    RS 33295-198; Zosuquidar trihydrochloride; LY335979; LY-335979; (R)-1-(4-((1aR,6s,10bS)-1,1-difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c][7]annulen-6-yl)piperazin-1-yl)-3-(quinolin-5-yloxy)propan-2-ol trihydrochloride
    
    CAS Number
    
    167465-36-3
    
    Molecular Formula
    
    C32H34Cl3F2N3O2
    
    Molecular Weight
    
    637.0
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in EtOH; ≥17.1 mg/mL in DMSO; ≥31.9 mg/mL in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Morad SA, Davis TS, et al. "Role of P-glycoprotein inhibitors in ceramide-based therapeutics for treatment of cancer." Biochem Pharmacol. 2017 Apr 15;130:21-33. PMID:28189725

LY335979 (Zosuquidar 3HCL)

LY335979 (Zosuquidar 3HCL)

Background

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