Tariquidar , 98% , 206873-63-4

Synonym(s):
N-[2-[[[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarboxamide;XR 9576;XR9576

CAS NO.：206873-63-4

Empirical Formula: C38H38N4O6

Molecular Weight: 646.73

MDL number: MFCD09837824

PRODUCT Properties

• Melting point: >190oC (dec.)
• Boiling point: 716.0±60.0 °C(Predicted)
• Density: 1.276±0.06 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: DMSO (Slightly), Methanol (Slightly)
• pka: 10.67±0.70(Predicted)
• form: powder
• color: white to light brown
• InChIKey: LGGHDPFKSSRQNS-UHFFFAOYSA-N
• SMILES: N1C2C(=CC=CC=2)C=C(C(NC2=CC(OC)=C(OC)C=C2C(NC2=CC=C(CCN3CCC4=C(C3)C=C(OC)C(OC)=C4)C=C2)=O)=O)C=1

Description and Uses

Tariquidar is an anthranilic acid derivative that binds to P-glycoprotein (K_d = 5.1 nM) and inhibits transport activity. It inhibits transport of vinblastine and paclitaxel in multidrug resistant CH^rB30 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.

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.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H315-H319
• Precautionary statements: P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313