|ENMD-2076 L-(+)-Tartaric acid Catalog No.GC12145|
Sample solution is provided at 25 µL, 10mM.
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Recombinant Aurora A and B kinase enzymes assays are carried out in kinase assay buffer (50 mM of HEPES, pH 7.5, 10 mM of MgCl2, 5 mM of EGTA, 0.05% Brij-35) supplemented with 2 mM of DTT. Activities are determined at an ATP concentration equivalent to the apparent Km for each enzyme, and an enzyme concentration that results in approximately 30% phosphorylation of the peptide substrate after 1 hour. Dose–response curves of relative enzyme activity versus ENMD-2076 concentration are plotted with Grafit and used to calculate IC50 values.
The antiproliferative effect of ENMD-2076 on adherent tumor cell lines is measured by plating 500 cells per well in a 96-well plate and incubating with 9 doses of compound, spanning 0.3 nM to 125 mM, for 96 hours. Cellular proliferation is measured using the sulforhodamine B assay.
Mice: Cell lines are injected subcutaneously or into the mammary fat pad (MDA-MB-231 only) of 5- to 6-week-old CB.17 SCID or NCr nude mice. Tumors are allowed to grow for 10 to 50 days before drug treatment. All treatments are with ENMD-2076 in water or ENMD-2076 free base in CMC-Tween vehicle (0.075% carboxymethylcellulose, 0.085% Tween 80 in water), administered orally. Percent tumor growth inhibition is calculated.
. Fletcher GC, et al. ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action. Mol Cancer Ther. 2011 Jan;10(1):126-37.
|Chemical Name||(E)-N-(5-methyl-1H-pyrazol-3-yl)-6-(4-methylpiperazin-1-yl)-2-styrylpyrimidin-4-amine 2,3-dihydroxysuccinate|
|Solubility||≥ 175.8 mg/mL in DMSO||Storage||Store at -20°C|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
|Shipping Condition||Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
ENMD-2076 is an orally bioavailable, small molecule inhibitor of Aurora kinases with IC50 values of 14nM and 350nM, respectively against Aurora Kinase A and Aurora Kinase B .
Besides Aurora kinases, ENMD-2076 inhibits multiple kinases involved in various cellular activities. Overexpression of Aurora Kinase A has been found in breast cancers and ENMD-2076 is thereby studied in breast cancers. It is reported that ENMD-2076 differentially inhibits 29 breast cancer cell lines with IC50 values ranged from 0.25 to 16.1μM. In the clonogenic assays, ENMD-2076 totally suppresses the colony formation in the sensitiveMDA-MB-468 cell line and decreases the formation in theHCC1806, SK-BR-3, and BT474 cell lines. ENMD-2076 is also reported to cause a G2 cell-cycle arrest at 1.25μM. Moreover, ENMD-2076 shows antitumor activity in TNBC xenograft models. Apart from the breast cancers, ENMD-2076 is developed in hematological malignancies therapy. The clinical trials have already conducted in Phase II [1, 2].
 Diamond JR, Eckhardt SG, Tan AC, Newton TP, Selby HM, Brunkow KL, Kachaeva MI, Varella-Garcia M, Pitts TM, Bray MR, Fletcher GC, Tentler JJ. Predictive biomarkers of sensitivity to the aurora and angiogenic kinase inhibitor ENMD-2076 in preclinical breast cancer models. Clin Cancer Res. 2013 Jan 1;19(1):291-303.
 How J, Yee K. ENMD-2076 for hematological malignancies. Expert Opin Investig Drugs. 2012 May;21(5):717-32.