Azd2171

The indazole derivative axitinib (AG-013736) is an orally available inhibitor of VEGFR, and also of the related PDGF and CSF-1 receptor TKs. This agent is in clinical development for head and neck and breast cancers, among others.30,31

HaC'

HaC'

Axitinib (AG-013736)

Other VEGFR inhibitors have been designed as analogues of the natural product staurosporine, a non-selective kinase inhibitor. For instance, CEP-5214, which was identified as the best candidate from SAR studies of about 2000 analogues, has a potent pan-VEGFR kinase inhibitory activity. Its N,N-dimethyl-glycine ester CEP-7055 is a water-soluble prodrug that can be orally administered and is undergoing clinical trials.32

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