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Motesanib

Motesanib is an inhibitor of VEGFR 1/2/3, PDGFR, c-Kit, and RET that displays anticancer chemotherapeutic and anti-angiogenic activities. In vivo, motesanib inhibits tumor growth of xenografts of various cancers. Motesanib is currently in clinical trials as a potential treatment for non-small cell lung cancer (NSCLC), breast cancer, and medullary thyroid cancer.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18945941

Cas No.

453562-69-1

Purity

≥98%

Formula

C22H23N5O

Formula Wt.

373.45

Chemical Name

N-(2,3-Dihydro-3,3-dimethyl-1H-indol-6-yl)-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide

IUPAC Name

N-(3,3-dimethyl-1,2-dihydroindol-6-yl)-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide

Synonym

AMG-706

Appearance

White to off white powder

Ellis PM, Al-Saleh K. Multitargeted anti-angiogenic agents and NSCLC: clinical update and future directions. Crit Rev Oncol Hematol. 2012 Oct;84(1):47-58. PMID: 22405734.

Coxon A, Ziegler B, Kaufman S, et al. Antitumor activity of motesanib alone and in combination with cisplatin or docetaxel in multiple human non-small-cell lung cancer xenograft models. Mol Cancer. 2012 Sep 19;11:70. PMID: 22992329.

Coxon A, Bready J, Kaufman S, et al. Anti-tumor activity of motesanib in a medullary thyroid cancer model. J Endocrinol Invest. 2012 Feb;35(2):181-90. PMID: 21422803.

Raghav KP, Blumenschein GR. Motesanib and advanced NSCLC: experiences and expectations. Expert Opin Investig Drugs. 2011 Jun;20(6):859-69. PMID: 21534718.

Polverino A, Coxon A, Starnes C, et al. AMG 706, an oral, multikinase inhibitor that selectively targets vascular endothelial growth factor, platelet-derived growth factor, and kit receptors, potently inhibits angiogenesis and induces regression in tumor xenografts. Cancer Res. 2006 Sep 1;66(17):8715-21. PMID: 16951187.

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