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ENMD-2076 is an orally-active, Aurora A/angiogenic kinase inhibitor with a unique kinase selectivity profile and multiple mechanisms of action. ENMD-2076 has been shown to inhibit a distinct profile of angiogenic tyrosine kinase targets in addition to the Aurora A kinase. ENMD-2076 also targets the VEGFR, Flt-3 and FGFR3 kinases which have been shown to play important roles in the pathology of several cancers. ENMD-2076 has shown promising activity in Phase 1 clinical trials in solid tumor cancers, leukemia, and multiple myeloma. ENMD-2076 is currently in a Phase 2 trial for ovarian cancer, and preclinical and clinical activities are ongoing in assessing the compound's applicability for other forms of cancer.
| Cell Experiment | |
|---|---|
| Cell lines | solid tumor cell lines and HUVECs, human leukemia cell lines |
| Preparation method | Cell and proliferative assays Cell lines were routinely tested for mycoplasma and used at low passage numbers (<10). The antiproliferative effect of ENMD-2076 on adherent tumor cell lines was measured by plating 500 cells per well in a 96-well plate and incubating with 9 doses of compound, spanning 0.3 nmol/L to 125 μmol/L, for 96 hours. Cellular proliferation was measured using the sulforhodamine B assay. The leukemia-derived, nonadherent cell lines were assayed by plating 5,000 cells per well in a 96-well plate. The cells were incubated with 9 doses of compound, spanning 0.3 nmol/L to 125 μmol/L, for 48 hours and then survival was assayed using the Alamar Blue reagent (M10350) according to the manufacturer’s instructions. To measure the effect of ENMD-2076 on VEGF- and fibroblast growth factor (FGF)-induced proliferation of human umbilical vein endothelial cell (HUVEC), cells were serum starved for 6 hours, then treated with ENMD-2076 free base, and stimulated with 5 ng/mL bFGF or 25 ng/mL VEGF for 72 hours. Cell proliferation was measured using WST-1 according to the manufacturer’s instructions. |
| Concentrations | 0.3 nM~125 μM |
| Incubation time | 48 or 96 h |
| Animal Experiment | |
|---|---|
| Animal models | MDA-MB-231 tumor xenograft model of 5- to 6-week-old CB.17 SCID or NCr nude mice |
| Formulation | ENMD-2076 in water or ENMD-2076 free base in CMC-Tween vehicle (0.075% carboxymethylcellulose, 0.085% Tween 80 in water) |
| Dosages | 75 or 302 mg/kg daily |
| Administration | orally |
| Molecular Weight | 525.56 |
| Formula | C25H31N7O6 |
| CAS Number | 934353-76-1 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] How et al. Expert Opin Investig Drugs. ENMD-2076 for hematological malignancies.
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| MLN8054
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