1744. Canertinib

Nomenclature

CAS number: 267243-28-7
N-[4-[(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]-6-quinazolinyl]-2-propenamide; N-[4-(3-chloro-4-fluorophenylamino)-7-(3-morpholin-4-ylpropoxy)quinazolin-6-yl]acrylamide.
C24H25ClFN5O3; mol wt 485.94.
C 59.32%, H 5.19%, Cl 7.30%, F 3.91%, N 14.41%, O 9.88%.

Description and references

Irreversible pan-erbB tyrosine kinase inhibitor. Prepn: A. J. Bridges et al., WO 0031048; eidem, US 6344455 (2000, 2002 both to Warner-Lambert); J. B. Smaill et al., J. Med. Chem. 43, 1380 (2000). Clinical pharmacokinetics in patients with solid malignancies: E. Calvo et al., Clin. Cancer Res. 10, 7112 (2004); and tolerability in refractory cancer: J. Nemunaitis et al., ibid. 11, 3846 (2005). Review of pharmacology and mechanism of action: L. F. Allen et al., Semin. Oncol. 30, Suppl. 16, 65-78 (2003); of development and clinical experience: C. M. Galmarini, IDrugs 7, 58-63 (2004).

Chemical structure

Properties

Crystals from methanol, mp 188-190°.

Derivative

Dihydrochloride.

Nomenclature

CAS number: 289499-45-2
CI-1033.
C24H25ClFN5O3.2HCl; mol wt 558.86.
C 51.58%, H 4.87%, Cl 19.03%, F 3.40%, N 12.53%, O 8.59%.

Properties

Sol in water.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic; Tyrosine Kinase Inhibitors