9939. Vatalanib

Nomenclature

CAS number: 212141-54-3
N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine; 1-(4-chloroanilino)-4-(4-pyridylmethyl)phthalazine; CGP-79787.
C20H15ClN4; mol wt 346.81.
C 69.26%, H 4.36%, Cl 10.22%, N 16.15%.

Description and 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).

Chemical structure

Properties

Crystals from water + diethyl ether, mp 209-212°.

Derivative

Succinate.

Nomenclature

CAS number: 212142-18-2
CGP-79787D; PTK-787; ZK-222584.
C20H15ClN4.C4H6O4; mol wt 464.90.
C 62.00%, H 4.55%, Cl 7.63%, N 12.05%, O 13.77%.

Properties

Crystals from ethanol, mp 195°.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic; Tyrosine Kinase Inhibitors