Date published: 2025-9-26

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Zosuquidar trihydrochloride (CAS 167465-36-3)

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Alternate Names:
LY335979; RS-33295-198
Application:
Zosuquidar trihydrochloride is a modulator of Pgp
CAS Number:
167465-36-3
Purity:
≥98%
Molecular Weight:
636.99
Molecular Formula:
C32H31F2N3O23HCl
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Zosuquidar trihydrochloride is a potent modulator of Mdr-1(P-glycoprotein-mediated multidrug resistance). This compound exhibits an IC50=60 nM. Zosuquidar trihydrochloride competitively inhibits equillibrium binding of drugs to Mdr-1 and shows an ability to reverse drug resistance to multiple oncolytics. Zosuquidar, also known as Zosuquidar trihydrochloride, is a powerful substance used in scientific research to examine the impact of P-glycoprotein (P-gp) inhibition on cellular processes. P-gp is a transmembrane protein responsible for expelling various drugs and molecules from cells. Zosuquidar acts as a substrate for P-gp and functions as a reversible inhibitor of this transporter. By binding to P-gp, Zosuquidar impedes its ability to pump drugs and molecules out of cells. This action results in elevated concentrations of drugs within the cells while reducing their levels outside the cells. As a consequence, Zosuquidar can enhance the effectiveness of drugs while minimizing their toxicity. Furthermore, Zosuquidar has been observed to modulate the activity of P-gp-dependent drug transporters, leading to alterations in the pharmacokinetics of drugs.


Zosuquidar trihydrochloride (CAS 167465-36-3) References

  1. A population pharmacokinetic model for doxorubicin and doxorubicinol in the presence of a novel MDR modulator, zosuquidar trihydrochloride (LY335979).  |  Callies, S., et al. 2003. Cancer Chemother Pharmacol. 51: 107-18. PMID: 12647011
  2. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice.  |  Kemper, EM., et al. 2004. Cancer Chemother Pharmacol. 53: 173-8. PMID: 14605863
  3. Bioanalysis of zosuquidar trihydrochloride (LY335979) in small volumes of human and murine plasma by ion-pairing reversed-phase high-performance liquid chromatography.  |  Kemper, EM., et al. 2003. J Chromatogr B Analyt Technol Biomed Life Sci. 798: 63-8. PMID: 14630360
  4. Population pharmacokinetic model for daunorubicin and daunorubicinol coadministered with zosuquidar.3HCl (LY335979).  |  Callies, S., et al. 2004. Cancer Chemother Pharmacol. 54: 39-48. PMID: 15045528
  5. Phase I study of docetaxel in combination with the P-glycoprotein inhibitor, zosuquidar, in resistant malignancies.  |  Fracasso, PM., et al. 2004. Clin Cancer Res. 10: 7220-8. PMID: 15534095
  6. Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats.  |  Anderson, BD., et al. 2006. Drug Metab Dispos. 34: 653-9. PMID: 16434546
  7. Modulation of the brain distribution of imatinib and its metabolites in mice by valspodar, zosuquidar and elacridar.  |  Bihorel, S., et al. 2007. Pharm Res. 24: 1720-8. PMID: 17380257
  8. Zosuquidar restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AML).  |  Tang, R., et al. 2008. BMC Cancer. 8: 51. PMID: 18271955
  9. Novel and emerging drugs for acute myeloid leukemia: pharmacology and therapeutic activity.  |  Robak, T., et al. 2011. Curr Med Chem. 18: 638-66. PMID: 21182488
  10. Zosuquidar and an albumin-binding prodrug of zosuquidar reverse multidrug resistance in breast cancer cells of doxorubicin and an albumin-binding prodrug of doxorubicin.  |  Abu Ajaj, K., et al. 2012. Breast Cancer Res Treat. 134: 117-29. PMID: 22228402
  11. Reversion of P-gp-Mediated Drug Resistance in Ovarian Carcinoma Cells with PHPMA-Zosuquidar Conjugates.  |  Battistella, C. and Klok, HA. 2017. Biomacromolecules. 18: 1855-1865. PMID: 28409628
  12. Structure of a zosuquidar and UIC2-bound human-mouse chimeric ABCB1.  |  Alam, A., et al. 2018. Proc Natl Acad Sci U S A. 115: E1973-E1982. PMID: 29440498
  13. Combinatorial Treatment of Birinapant and Zosuquidar Enhances Effective Control of HBV Replication In Vivo.  |  Morrish, E., et al. 2020. Viruses. 12: PMID: 32824616

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Zosuquidar trihydrochloride, 5 mg

sc-364314
5 mg
$138.00

Zosuquidar trihydrochloride, 10 mg

sc-364314A
10 mg
$330.00