Zosuquidar trihydrochloride

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Cat.No. 5456 - Zosuquidar trihydrochloride | C32H31F2N3O2.3HCl | CAS No. 167465-36-3
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: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

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Technical Data

M. Wt 636.99
Formula C32H31F2N3O2.3HCl
Storage Store at -20°C
Purity ≥98% (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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.85 50

Preparing Stock Solutions

The following data is based on the product molecular weight 636.99. Batch specific molecular weights may vary from batch to batch due to solvent 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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References

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


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Citations for Zosuquidar trihydrochloride

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