enmd-2076

ENMD‑2076 is an orally bioavailable synthetic small molecule with potential antiangiogenic and antineoplastic activities. It acts as a multi-targeted kinase inhibitor with selective activity against Aurora A kinase and several angiogenic tyrosine kinases such as VEGFR2 (KDR), VEGFR3 (Flt4), FGFR1/2/3. Inhibition of these targets may result in the inhibition of cell division and proliferation and may induce apoptosis in tumor cells that overexpress Aurora kinases; antiangiogenic activity is related to the inhibition of angiogenic tyrosine kinases[1][2][5]. Developed by Miikana Therapeutics and later by CASI Pharmaceuticals (formerly EntreMed), it has been investigated for various cancers including ovarian clear cell carcinoma (OCCC), triple-negative breast cancer (TNBC), soft tissue sarcoma (STS), acute myeloid leukemia (AML), multiple myeloma, liver cancer[5][8]. It has received orphan drug status for ovarian cancer, multiple myeloma, liver cancer and acute myeloid leukemia[5].

Other names

6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amineUNII-J6U9WP10T7UNII-J-6U9WP10T7UNII-J 6U9WP10T7DTXSID60239430DTXSID-60239430DTXSID 60239430DTXCID80161921DTXCID-80161921DTXCID 80161921934353-76-1