LY335979 (Zosuquidar 3HCL) (Synonyms: RS 33295-198; Zosuquidar trihydrochloride; LY335979; LY-335979) |
| Catalog No.GC16609 |
Le trichlorhydrate de zosuquidar (LY335979) est un inhibiteur de la glycoprotéine P (P-gp) (Ki = 59 nM). LY335979 (Zosuquidar 3HCL) présente des activités antitumorales et peut être utilisé dans la recherche sur la leucémie myéloÏde aiguë (LMA).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 167465-36-3
Sample solution is provided at 25 µL, 10mM.
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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].
References:
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.
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