CEP-11981

CEP-11981 is an orally bioavailable small molecule inhibitor of multiple receptor tyrosine kinases involved in angiogenesis and tumor growth. It selectively targets vascular endothelial growth factor receptor 1 (VEGFR1), vascular endothelial growth factor receptor 2 (VEGFR2), vascular endothelial growth factor receptor 3 (VEGFR3), Tie2 receptor tyrosine kinase, fibroblast growth factor receptor 1 (FGFR1), as well as proto-oncogene c-SRC. By inhibiting these kinases, CEP-11981 disrupts endothelial cell migration, proliferation and survival—key processes in tumor angiogenesis—and thereby inhibits tumor cell proliferation and induces tumor cell death. The drug was developed for antiangiogenic and antineoplastic activity in various solid tumors including prostate cancer, adenocarcinoma of the prostate, neuroendocrine gastroenteropancreatic tumors, pancreatic cancer and urothelial carcinoma. Clinical development reached Phase II but has since been discontinued[1][2][3][4][5][6][7][8].

Other names

11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo(5,4-a)pyrrolo(3,4-c)carbazol-4-oneJ8AY0Z4CBPJ-8AY0Z4CBPJ 8AY0Z4CBP