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ENMD-2076 L-(+)-Tartaric acid

Aurora kinases inhibitor CAS# 1291074-87-7

ENMD-2076 L-(+)-Tartaric acid

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Quality Control of ENMD-2076 L-(+)-Tartaric acid

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ENMD-2076 L-(+)-Tartaric acid

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Chemical Properties of ENMD-2076 L-(+)-Tartaric acid

Cas No. 1291074-87-7 SDF Download SDF
PubChem ID 24776050 Appearance Powder
Formula C25H31N7O6 M.Wt 525.56
Type of Compound N/A Storage Desiccate at -20°C
Solubility 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL
Chemical Name (2R,3R)-2,3-dihydroxybutanedioic acid;6-(4-methylpiperazin-1-yl)-N-(5-methyl-1H-pyrazol-3-yl)-2-[(E)-2-phenylethenyl]pyrimidin-4-amine
SMILES CC1=CC(=NN1)NC2=NC(=NC(=C2)N3CCN(CC3)C)C=CC4=CC=CC=C4.C(C(C(=O)O)O)(C(=O)O)O
Standard InChIKey KGWWHPZQLVVAPT-STTJLUEPSA-N
Standard InChI InChI=1S/C21H25N7.C4H6O6/c1-16-14-20(26-25-16)23-19-15-21(28-12-10-27(2)11-13-28)24-18(22-19)9-8-17-6-4-3-5-7-17;5-1(3(7)8)2(6)4(9)10/h3-9,14-15H,10-13H2,1-2H3,(H2,22,23,24,25,26);1-2,5-6H,(H,7,8)(H,9,10)/b9-8+;/t;1-,2-/m.1/s1
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.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ENMD-2076 L-(+)-Tartaric acid

DescriptionENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.In Vitro:ENMD-2076 is selective toward Aurora A versus Aurora B (IC50=350 nM). ENMD-2076 inhibits HUVEC growth with an IC50 value of 0.15 mM. Against 10 human leukemia cell lines, the IC50 values range from 0.025 to 0.53 mM. Within this panel, MV4:11 cells are the most sensitive cells by a factor of greater than 4. The lymphoma-derived U937 cell line treated with ENMD-2076 shows that the ENMD-2076 induces a dose-dependent increase in G2-M-phase arrest as well as the induction of apoptosis. ENMD-2076 inhibits cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation in THP-1 cells, which have been shown to express FL-responsive wild-type Flt- 3 (18) with an IC50 value of 28 nM. ENMD-2076 inhibits stem cell factor (SCF)-induced Kit autophosphorylation in MO7e cells with an IC50 value of 40 nM. ENMD-2076 inhibits VEGFR2/KDR autophosphorylation with an IC50 value of 7 nM[1].In Vivo:ENMD-2076 treatment results in statistically significant, dose dependent inhibition of tumor growth or tumor regression. Moreover, there is no correlation between tumor growth rate and antitumor efficacy, which would conceivably be expected for a mitotic kinase inhibitor, as fast growing (e.g., A375 melanoma) and slow-growing (e.g., HT29 colon carcinoma) tumors are similarly inhibited by ENMD-2076. ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), with no weight loss or signs of morbidity noted in any study at this dose with the exception of the A375 model[1].

References:
[1]. 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. [2]. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25.

Protocol

Kinase Assay [1]
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[1].

Cell Assay [1]
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[1].

Animal Administration [1]
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[1].

References:
[1]. 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. [2]. Wang X, et al. Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma. Br J Haematol. 2010 Aug;150(3):313-25.

ENMD-2076 L-(+)-Tartaric acid Dilution Calculator

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ENMD-2076 L-(+)-Tartaric acid Molarity Calculator

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Preparing Stock Solutions of ENMD-2076 L-(+)-Tartaric acid

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9027 mL 9.5137 mL 19.0273 mL 38.0546 mL 47.5683 mL
5 mM 0.3805 mL 1.9027 mL 3.8055 mL 7.6109 mL 9.5137 mL
10 mM 0.1903 mL 0.9514 mL 1.9027 mL 3.8055 mL 4.7568 mL
50 mM 0.0381 mL 0.1903 mL 0.3805 mL 0.7611 mL 0.9514 mL
100 mM 0.019 mL 0.0951 mL 0.1903 mL 0.3805 mL 0.4757 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on ENMD-2076 L-(+)-Tartaric acid

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 [1].

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].

References:
[1] 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.
[2] How J, Yee K. ENMD-2076 for hematological malignancies. Expert Opin Investig Drugs. 2012 May;21(5):717-32.

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Description

ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

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