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Tariquidar methanesulfonate hydrate

Chemical Structure : Tariquidar methanesulfonate hydrate

CAS No.: 625375-83-9

Tariquidar methanesulfonate hydrate (XR 9576;XR-9576;XR9576)

Catalog No.: PC-42649Not For Human Use, Lab Use Only.

A potent, specific P-gp inhibitor with Kd of 5.1 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

A potent, specific P-gp inhibitor with Kd of 5.1 nM; potentiates the cytotoxicity of several drugs including doxorubicin, paclitaxel, etoposide, and vincristine in a panel of human MDR cell lines at 25-80 nM; exhibits potent i.v. and p.o. activity without apparently enhancing the plasma pharmacokinetics of paclitaxel or the toxicity of coadministered drugs.

Breast Cancer

Phase 2 Discontinued

Physicochemical Properties

M.Wt 892.9887
Formula C40H52N4O15S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 296 mg/mL; H2O: < 8.9 mg/mL

Chemical Name/SMILES

3-Quinolinecarboxamide, N-[2-[[[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-, methanesulfonate, hydrate (1:2:3)

References

1. Martin C, et al. Br J Pharmacol. 1999 Sep;128(2):403-11.

2. Mistry P, et al. Cancer Res. 2001 Jan 15;61(2):749-58.

3. Walker J, et al. Eur J Cancer. 2004 Mar;40(4):594-605.

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