10304. Axitinib

Nomenclature

CAS number: 319460-85-0
N-Methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide; AG-013736.
C22H18N4OS; mol wt 386.47.
C 68.37%, H 4.69%, N 14.50%, O 4.14%, S 8.30%.

Description and references

Receptor tyrosine kinase inhibitor of VEGFR, PDGFR, and c-KIT; induces anti-angiogenic response. Prepn: R. S. Kania et al., WO 0102369; eidem, US 6534524 (2001, 2003 both to Agouron). Anti-angiogenic activity in breast cancer xenografts: L. J. Wilmes et al., Magn. Reson. Imaging 25, 319 (2007) DOI PubMed. In vivo effect in combination with cyclophosphamide: J. Ma, D. J. Waxman, Mol. Cancer Ther. 7, 79 (2008) DOI PubMed. Clinical pharmacokinetics in advanced solid tumors: H. S. Rugo et al., J. Clin. Oncol. 23, 5474 (2005) DOI PubMed. Clinical evaluation in renal cell carcinoma: O. Rixe et al., Lancet Oncol. 8, 975 (2007) DOI PubMed. Review of clinical experience in renal cell carcinoma: D. J. George, Clin. Cancer Res. 13, Suppl. 2, 753s-757s (2007) DOI PubMed; G. Sonpavde et al., Expert Opin. Invest. Drugs 17, 741-748 (2008) DOI PubMed.

Chemical structure

Properties

Sol in aq methanol.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic; Tyrosine Kinase Inhibitors