ENMD-2076

ENMD-2076

CAT N°: 22956
Price:

From 75.00 63.75

ENMD-2076 is a multi-kinase inhibitor that inhibits FMS-related tyrosine kinase 3 (FLT3), RET, and Aurora A kinase with IC50 values of 1.86, 10.4, and 14 nM, respectively.{39604} It inhibits additional kinases involved in angiogenesis such as VEGFR3, PDGFR?, and FGFR2, among others, with IC50 values of less than 100 nM. It inhibits proliferation of several human triple-negative breast cancer (TNBC) cell lines with IC50 values of less than 1 µM, halts the cell cycle at the G2 phase, and induces apoptosis.{39603} Oral administration of ENMD-2076 (200 mg/kg), reduces proliferation, enhances p53- and p73-mediated cancer cell apoptosis and senescence, and inhibits growth of sensitive primary tumors in a TNBC mouse xenograft model.{39605} It also decreases tumor vascular permeability and perfusion and inhibits tumor growth in human TNBC and colorectal cancer mouse xenograft models when administered orally at a dose of 100 mg/kg.{39603,39606}

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