Title: Vatalanib
CAS Registry Number: 212141-54-3
CAS Name: N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine
Additional Names: 1-(4-chloroanilino)-4-(4-pyridylmethyl)phthalazine
Manufacturers' Codes: CGP-79787
Molecular Formula: C20H15ClN4
Molecular Weight: 346.81
Percent Composition: C 69.26%, H 4.36%, Cl 10.22%, N 16.15%
Literature References: Vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor; vascular endothelial angiogenesis inhibitor. Prepn: G. Bold et al., WO 9835958; eidem, US 6258812 (1998, 2001 both to Novartis); eidem, J. Med. Chem. 43, 2310 (2000). Enzyme inhibition study and pharmacology: J. M. Wood et al., Cancer Res. 60, 2178 (2000). Antiangiogenic activity: J. Drevs et al., ibid. 62, 4015 (2002). Clinical pharmacokinetics: B. Morgan et al., J. Clin. Oncol. 21, 3955 (2003). Review of mechanism of action: P. Furet, P. W. Manley ACS Symp. Ser. 796, 282-298 (2001); and therapeutic potential: A. L. Thomas et al., Semin. Oncol. 30, Suppl. 6, 32-38 (2003).
Properties: Crystals from water + diethyl ether, mp 209-212°.
Melting point: mp 209-212°
Derivative Type: Succinate
CAS Registry Number: 212142-18-2
Manufacturers' Codes: CGP-79787D; PTK-787; ZK-222584
Molecular Formula: C20H15ClN4.C4H6O4
Molecular Weight: 464.90
Percent Composition: C 62.00%, H 4.55%, Cl 7.63%, N 12.05%, O 13.77%
Properties: Crystals from ethanol, mp 195°.
Melting point: mp 195°
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Tyrosine Kinase Inhibitors. |