Chemical Property of Tariquidar
Chemical Property:
- Vapor Pressure:2.37E-20mmHg at 25°C
- Boiling Point:716°Cat760mmHg
- PKA:10.67±0.70(Predicted)
- Flash Point:386.8°C
- PSA：111.25000
- Density:1.276g/cm3
- LogP:6.45850
- Storage Temp.:2-8°C
- Solubility.:DMSO (Slightly), Methanol (Slightly)
- XLogP3:6.1
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:8
- Rotatable Bond Count:11
- Exact Mass:646.27913494
- Heavy Atom Count:48
- Complexity:1040
- Purity/Quality:
-
99%, *data from raw suppliers
Tariquidar *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:COC1=C(C=C2CN(CCC2=C1)CCC3=CC=C(C=C3)NC(=O)C4=CC(=C(C=C4NC(=O)C5=CC6=CC=CC=C6N=C5)OC)OC)OC
- Recent ClinicalTrials:Phase I Trial of Tariquidar (XR9576) in Combination With Doxorubicin, Vinorelbine, or Docetaxel in Pediatric Patients With Solid Tumors
- Recent EU Clinical Trials:A pilot study to assess the influence of drug transporters on brain and organ distribution of erlotinib in humans
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Description
Tariquidar is an anthranilic acid derivative that binds to P-glycoprotein (Kd = 5.1 nM) and inhibits transport activity. It inhibits transport of vinblastine and paclitaxel in multidrug resistant CHrB30 cells, increasing the steady state accumulation to non-P-glycoprotein-expressing multidrug sensitive cell levels (EC50 = 487 nM). Tariquidar also enhances the distribution of its substrates, increasing the amount of substrate entering the CNS. When administered at doses of 2 and 6.25 mg/kg in mice in combination with the peripherally-restricted opioid loperamide, the latency to paw withdrawal in a hot plate assay increases, indicating that loperamide is transported into the CNS.
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Uses
Tariquidar is a p-glycoprotein drug efflux pump inhibitor. Tariquidar inhibits the ATPase activity of P-glycoprotein, suggesting that the modulating effect is derived from the inhibition of substrate
binding, inhibition of ATP hydrolysis or both.Tariquidar can be considered an ideal agent for testing the role of P-glycoprotein inhibition in cancer Tariquidar is a p-glycoprotein drug efflux pump inhibitor. Tariquidar inhibits the ATPase activity of P-glycoprotein, suggesting that the modulating effect is derived from the inhibition of substrate binding, inhibition of ATP hydrolysis or both.Tariquidar can be considered an ideal agent for testing the role of P-glycoprotein inhibition in cancer.
