CEP-5214 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase, derived from an indenopyrrolocarbazole template. With an IC50 value of 8 nM against VEGF-R2, it demonstrates remarkable selectivity over other kinases, exhibiting low-nanomolar inhibition (IC50 of 4 nM). This compound has shown significant antitumor activity in both cellular and in vivo models, and it has advanced to phase I clinical trials in the form of a water-soluble prodrug (CEP-7055) to improve oral bioavailability. Its distinctive mechanism of action makes it valuable for research applications related to cancer and angiogenesis.
CEP-5214 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2) tyrosine kinase, derived from an indenopyrrolocarbazole template. With an IC50 value of 8 nM against VEGF-R2, it demonstrates remarkable selectivity over other kinases, exhibiting low-nanomolar inhibition (IC50 of 4 nM). This compound has shown significant antitumor activity in both cellular and in vivo models, and it has advanced to phase I clinical trials in the form of a water-soluble prodrug (CEP-7055) to improve oral bioavailability. Its distinctive mechanism of action makes it valuable for research applications related to cancer and angiogenesis.
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