9064. Tariquidar

Nomenclature

CAS number: 206873-63-4
N-[2-[[[4-[2-(3,4-Dihydro-6,7-dimethoxy-2(1H)-isoquinolinyl)ethyl]phenyl]amino]carbonyl]-4,5-dimethoxyphenyl]-3-quinolinecarboxamide; XR-9576.
C38H38N4O6; mol wt 646.73.
C 70.57%, H 5.92%, N 8.66%, O 14.84%.

Description and references

Multidrug resistance modulator; selective inhibitor of P-glycoprotein (P-gp), q.v. Prepn: H. Ryder et al., WO 9817648; eidem, US 6218393 (1998, 2001 both to Xenova); M. Roe et al., Bioorg. Med. Chem. Lett. 9, 595 (1999). Molecular interaction with P-gp: C. Martin et al., Br. J. Pharmacol. 128, 403 (1999). Effect on multidrug resistant cell lines: P. Mistry et al., Cancer Res. 61, 749 (2001). Clinical pharmacology: A. Stewart et al., Clin. Cancer Res. 6, 4186 (2000). Effect on accumulation of 99mTc-sestamibi, q.v., in patients with metastatic cancers: M. Agrawal et al., Clin. Cancer Res. 9, 650 (2003).

Chemical structure

Therapeutic Category

Antineoplastic adjunct (chemosensitizer).

Keywords

Antineoplastic Adjunct; Chemosensitizer