10338. Motesanib

Nomenclature

CAS number: 453562-69-1
N-(2,3-Dihydro-3,3-dimethyl-1H-indol-6-yl)-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide.
C22H23N5O; mol wt 373.45.
C 70.76%, H 6.21%, N 18.75%, O 4.28%.

Description and references

Multikinase inhibitor that targets VEGF, PDGF, and Kit receptor tyrosine kinases; inhibits angiogenesis in solid tumors. Prepn: G. Chen et al., WO 02066470; B. Askew et al., US 6878714 (2002, 2005 both to Amgen); of pharmaceutical salt forms: B. B. Liu et al., WO 07087026; G. Alva et al., WO 07092178 (both 2007 to Amgen). Kinase inhibition and bioactivity: A. Polverino et al., Cancer Res. 66, 8715 (2006) DOI PubMed. Clinical pharmacokinetics: L. S. Rosen et al., J. Clin. Oncol. 25, 2369 (2007) DOI PubMed. Clinical trial in thyroid cancer: S. I. Sherman et al., N. Engl. J. Med. 359, 31 (2008) DOI PubMed.

Chemical structure

Derivative

Diphosphate.

Nomenclature

CAS number: 857876-30-3
AMG-706.
C22H23N5O.2H3PO4; mol wt 569.44.
C 46.40%, H 5.13%, N 12.30%, O 25.29%, P 10.88%.

Properties

Crystalline solid, mp 215° (dec). Forms stable monophosphate dihydrate in boiling water.

Therapeutic Category

Antineoplastic.

Keywords

Antineoplastic; Tyrosine Kinase Inhibitors