Cabozantinib

CAT#: H200595

CAS#: 849217-68-1

Description: Cabozantinib, also known as XL-184 or BMS-907351, is an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Cabozantinib strongly binds to and inhibits several tyrosine receptor kinases. Specifically, cabozantinib appears to have a strong affinity for the hepatocyte growth factor receptor (Met) and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in inhibition of tumor growth and angiogenesis, and tumor regression. Cabozantinib was approved by the U.S. FDA in November 2012 for the treatment of medullary thyroid cancer.

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Synthetic Routes

Cabozantinib - Synthetic Route 1

Cabozantinib route01

Synthetic reference

Laus, Gerhard; Schreiner, Erwin; Nerdinger, Sven; Kahlenberg, Volker; Wurst, Klaus; Vergeiner, Stefan; Schottenberger, Herwig. Crystal structures of intermediates in a new synthesis of antitumor drug cabozantinib. Heterocycles. Volume 93. Issue 1, Spec. Issue. Pages 323-332. Journal; Online Computer File. (2016).

Cabozantinib - Synthetic Route 2

Cabozantinib route02

Synthetic reference

Lien, Vegard Torp; Klaveness, Jo; Olberg, Dag Erlend. One-step synthesis of [18F]cabozantinib for use in positron emission tomography imaging of c-Met. Journal of Labelled Compounds and Radiopharmaceuticals. Volume 61. Issue 1. Pages 11-17. Journal; Online Computer File. (2018).

Cabozantinib - Synthetic Route 3

Cabozantinib route03

Synthetic reference

Xu, Wei; Donnelly, David J.; Chow, Patrick L.; Henley, Benjamin J. Method of preparing fluorine-18 labeled cabozantinib and its analogs. Assignee Exelixis, Inc., USA. WO 2016019285. (2016).

Cabozantinib - Synthetic Route 4

Cabozantinib route04

Synthetic reference

Shi, Xiangfei; Zhao, Rui; Meng, Qingyi; Zhang, Xiquan. Process for the preparation of cabozantinib and its intermediate. Assignee Chia Tai Tianqing Pharmaceutical Group Co., Ltd., Peop. Rep. China. CN 103664776. (2014).

Cabozantinib - Synthetic Route 5

Cabozantinib route05

Synthetic reference

Wang, Zhiguo; Song, Yanhong; Ma, Xiujuan; Tian, Beibei; Li, Shijiang; Li, Chao; Li, Tao; Zhang, Xin. Preparation method of Cabozantinib from diethyl malonate and 4-fluoroaniline. Assignee Shanghai Zaiqi Bio-Tech Co., Ltd., Peop. Rep. China. CN 106632028. (2015).

Cabozantinib - Synthetic Route 6

Cabozantinib route06

Synthetic reference

Wang, Kunpeng; Han, Yuelin. New preparation method of cabozantinib. Assignee Nanjing Finetech Chemical Co., Ltd., Peop. Rep. China. CN 110240563. (2019).