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Cabozantinib

Cabozantanib is an anticancer chemotherapeutic compound that has been approved to treat medullary thyroid cancer and is in clinical trials as a treatment for other types of solid tumors. Cabozantanib exerts its anticancer activity through inhibition of Met, RET, and VEGFR2, increasing apoptosis and inhibiting cell growth and osteoclast proliferation in vitro and in vivo.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18846087

Cas No.

849217-68-1

Purity

≥98%

Formula

C28H24FN3O5

Formula Wt.

501.51

Chemical Name

N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

IUPAC Name

1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Synonym

XL-184, BMS-907351

Solubility

Soluble in DMSO (≥117mg/mL), insoluble in water (≤1 mg/mL).

Appearance

White to off white powder

Dai J, Zhang H, Karatsinides A, et al. Cabozantinib inhibits prostate cancer growth and prevents tumor-induced bone lesions. Clin Cancer Res. 2013 Oct 4. [Epub ahead of print]. PMID: 24097861.

Elisei R, Schlumberger MJ, Müller SP, et al. Cabozantinib in progressive medullary thyroid cancer. J Clin Oncol. 2013 Oct 10;31(29):3639-46. PMID: 24002501.

Bentzien F, Zuzow M, Heald N, et al. In Vitro and In Vivo Activity of Cabozantinib (XL184), an Inhibitor of RET, MET, and VEGFR2, in a Model of Medullary Thyroid Cancer. Thyroid. 2013 Sep 17. [Epub ahead of print]. PMID: 23705946.

Navis AC, Bourgonje A, Wesseling P, et al. Effects of dual targeting of tumor cells and stroma in human glioblastoma xenografts with a tyrosine kinase inhibitor against c-MET and VEGFR2. PLoS One. 2013;8(3):e58262. PMID: 23484006.

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