ENMD-2076 L-(+)-Tartaric acidAurora kinases inhibitor CAS# 1291074-87-7 |
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
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. |
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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. |
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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. |
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.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: |
ENMD-2076 L-(+)-Tartaric acid Dilution Calculator
ENMD-2076 L-(+)-Tartaric acid Molarity Calculator
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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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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