Tariquidar
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Tariquidar
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CAS No:
206873-63-4
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Formula:
C38H38N4O6
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Chemical Name:
Tariquidar
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Synonyms:
3-Quinolinecarboxamide,N-[2-[[[4-[2-(3,4-dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-;N-[2-[[[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarboxamide;XR 9576;Tariquidar
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CAS No:
Description
Tariquidar is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1±0.9 nM).
Tariquidar is a member of benzamides.|Tariquidar is an anthranilamide derivative with multidrug resistance properties. Tariquidar non-competitively binds to the p-glycoprotein transporter, thereby inhibiting transmembrane transport of anticancer drugs. Inhibition of transmembrane transport may result in increased intracellular concentrations of an anticancer drug, thereby augmenting its cytotoxicity. (NCI04)
Drug Information
Investigated for use/treatment in ovarian cancer, lung cancer, and breast cancer.
Tariquidar is an anthranilic acid derivative third generation P-glycoprotein (P-gp) inhibitors. P-gp is a transport protein found in normal cells that has many trasport and modulatory functions, from affecting the distribution and bioavailability of drugs to mediating the migration of dendritic cells. P-gp is responsible for multidrug resistance through transport of anti-cancer drugs out of their target cells. It is proposed that tariquidar's and its derivatives may bind to the H-binding site of P-gp through multiple mechanisms of binding.
tariquidar
Tariquidar Use and Manufacturing
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
Human drugs -> Rare disease (orphan)
Computed Properties
Molecular Weight:646.7
XLogP3:6.1
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:8
Rotatable Bond Count:11
Exact Mass:646.27913494
Monoisotopic Mass:646.27913494
Topological Polar Surface Area:111
Heavy Atom Count:48
Complexity:1040
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes
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