Sunday, January 18, 2015

Cabozantinib



Common name: Cabozantinib; XL184; Cometriq; BMS-907351; Cabozantinib L-Malate; Cabozantinib S-Malate
Trademarks:  Cometriq
Molecular Formula: C28H24FN3O5 
CAS Registry Number: 849217-68-1
CAS Name: N-(4-((6,7-Dimethoxyquinolin-4-yl)oxy)phenyl)-N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide
Molecular Weight: 501.51
Activity: Tyrosine Kinase Inhibitor; Protein Kinase Inhibitor;  c-Met Kinase Inhibitor; VEGFR2 Kinase Inhibitor; KDR Kinase Inhibitor; Anti-angiogenesis Therapy

Cabozantinib synthesis: WO2005030140A2 (revisited in Ref. 3)



References:
1. Bannen, L. C.; et. al. C-met modulators and methods of use. WO2005030140A2
2. Gallagher, W. P.; et. al. Malate salt of n-(4-{ [ 6,7-bis(methyloxy)quinolin-4-yl] oxy}phenyl-n'-(4-fluorophenyl) cyclopropane-1-dicarboxamide, and crystalline forms therof for the treatment of cancer. WO2010083414A1
3. Wilson, J. A.; et. al. Process for preparing quinoline derivatives. WO2013059788A1
4. Yakes, F. M.; et. al. Cabozantinib (XL184), a Novel MET and VEGFR2 Inhibitor, Simultaneously Suppresses Metastasis, Angiogenesis, and Tumor Growth. Mol Cancer Ther 2011, 10(12), 2298-308. (activity)