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Tariquidar

Tariquidar structure

CAS No:
206873-63-4
Formula:
C38H38N4O6
Chemical Name:
Tariquidar
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
Categories:
Biochemical Engineering > Inhibitors

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)

Tariquidar Basic Attributes

Molecular Weight：

646.73

Exact Mass：

646.73

UNII：

J58862DTVD

DSSTox ID：

DTXSID10174746

NCI Thesaurus Code：

C2246

HScode：

2933499090

Characteristics

PSA：

111

XLogP3：

6.1

Density：

1.3±0.1 g/cm3

Boiling Point：

716°C at 760 mmHg

Flash Point：

386.8±32.9 °C

Refractive Index：

1.662

Vapor Pressure：

2.37E-20mmHg at 25°C

Drug Information

Drug Indication：

Investigated for use/treatment in ovarian cancer, lung cancer, and breast cancer.

Mechanism of Action：

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.

MeSH Entry Terms：

tariquidar

Tariquidar Use and Manufacturing

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

Use Classification：

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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Tariquidar

CAS No.: 206873-63-4

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