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Submit ReviewZosuquidar trihydrochloride
Description: High affinity P-gp inhibitor
Alternative Names: LY 335979
Chemical Name: (αR)-4-[(1aα,6α,10bα)-1,1-Difluoro-1,1a,6,10b-tetrahydrodibenzo[a,e]cyclopropa[c]cyclohepten-6-yl]-α-[(5-quinolinyloxy)methyl]-1-piperazineethanol trihydrochloride
Purity: ≥97% (HPLC)
Biological Activity for Zosuquidar trihydrochloride
Zosuquidar trihydrochloride is a high affinity P-glycoprotein (P-gp) inhibitor (Kd = 79 nM). Restores doxorubicin (Cat. No. 2252) sensitivity in P-gp-expressing multidrug (MDR) resistant cancer cell lines. Also potentiates antitumor efficacy of taxol (Cat. No. 1097) in a MDR human non-small cell lung carcinoma xenograft mouse model.
Compound Libraries for Zosuquidar trihydrochloride
Zosuquidar trihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Zosuquidar trihydrochloride
| M. Wt | 636.99 |
| Formula | C32H31F2N3O2.3HCl |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 167465-36-3 |
| PubChem ID | 153997 |
| InChI Key | ZPFVQKPWGDRLHL-ZLYBXYBFSA-N |
| Smiles | F[C@@]2(F)[C@H]1C3=C(C=CC=C3)[C@H](N5CCN(C[C@H](COC6=CC=CC7=C6C=CC=N7)O)CC5)C4=C(C=CC=C4)[C@H]12.Cl.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Zosuquidar trihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 31.85 | 50 |
Preparing Stock Solutions for Zosuquidar trihydrochloride
The following data is based on the product molecular weight 636.99. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 3.14 mL | 15.7 mL | 31.4 mL |
| 2.5 mM | 0.63 mL | 3.14 mL | 6.28 mL |
| 5 mM | 0.31 mL | 1.57 mL | 3.14 mL |
| 25 mM | 0.06 mL | 0.31 mL | 0.63 mL |
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Product Datasheets for Zosuquidar trihydrochloride
References for Zosuquidar trihydrochloride
References are publications that support the biological activity of the product.
Dantzig et al (1999) Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities. J.Pharmacol.Exp.Ther. 290 854 PMID: 10411602
Dantzig et al (1996) Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979. Cancer Res. 56 4171 PMID: 8797588
If you know of a relevant reference for Zosuquidar trihydrochloride, please let us know.
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Keywords: Zosuquidar trihydrochloride, Zosuquidar trihydrochloride supplier, LY335979, RS33295198, high, affinity, p-glycoprotein, p-gp, inhibitors, inhibits, multidrug, transporters, resistance, LY, 335979, Multidrug, Transporters, 5456, Tocris Bioscience
3 Citations for Zosuquidar trihydrochloride
Citations are publications that use Tocris products. Selected citations for Zosuquidar trihydrochloride include:
Troy et al (2021) A genome-wide CRISPR/Cas9 screen in acute myeloid leukemia cells identifies regulators of TAK-243 sensitivity. JCI Insight 6 PMID: 33476303
Dalia et al (2022) Combinatorial Anticancer Drug Screen Identifies Off-Target Effects of Epigenetic Chemical Probes. ACS Chem Biol 17 2801-2816 PMID: 36084291
Terrance G et al (2019) Lower Tubulin Expression in Glioblastoma Stem Cells Attenuates Efficacy of Microtubule-Targeting Agents. ACS Pharmacol Transl Sci 2 402-413 PMID: 32259073
Do you know of a great paper that uses Zosuquidar trihydrochloride from Tocris? Please let us know.
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