| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Aurora A 1.86 nM (IC50) KDR 58.2 nM (IC50) Flt-4 15.9 nM (IC50) FGFR1 92.7 nM (IC50) FGFR2 70.8 nM (IC50) PDGFRα 56.4 nM (IC50) Flt3 14 nM (IC50)
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|---|---|
| ln Vitro |
With an IC50 of 350 nM, ENMD-2076 exhibits selectivity toward Aurora A over Aurora B. HUVEC growth is inhibited by ENMD-2076, with an IC50 value of 0.15 mM. The IC50 values against ten human leukemia cell lines span from 0.025 to 0.53 mM. The most sensitive cells in this panel by a factor larger than four are MV4:11 cells. The ENMD-2076 treatment of the lymphoma-derived U937 cell line results in a dose-dependent increase in G2-M-phase arrest and apoptosis induction. With an IC50 value of 28 nM, ENMD-2076 suppresses Flt3 autophosphorylation induced by cellular Flt3 ligand (FL) in THP-1 cells, which express FL-responsive wild-type Flt-3 (18). With an IC50 value of 40 nM, ENMD-2076 prevents Kit autophosphorylation in MO7e cells caused by stem cell factor (SCF). With an IC50 value of 7 nM, ENMD-2076 inhibits VEGFR2/KDR autophosphorylation[1].
|
| ln Vivo |
Tumor growth or regression is statistically significantly and dose-dependently inhibited by ENMD-2076 treatment. Additionally, there is no association between the rate of tumor growth and the effectiveness of the antitumor treatment, which is not surprising for a mitotic kinase inhibitor given that ENMD-2076 inhibits both slow-growing (such as HT29 colon carcinoma) and fast-growing (like A375 melanoma) tumors. With the exception of the A375 model, ENMD-2076 is well tolerated at daily doses up to 302 mg/kg (equivalent to 200 mg/kg of the free base), and no weight loss or morbidity symptoms have been observed in any study at this dose[1].
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| 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 |
| Molecular Formula |
C25H31N7O6
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|---|---|
| Molecular Weight |
525.56
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| CAS # |
1453868-32-0
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| Related CAS # |
ENMD-2076;934353-76-1
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| SMILES |
O[C@@H](C(=O)O)[C@H](C(=O)O)O.N1(C2C=C(NC3C=C(C)NN=3)N=C(/C=C/C3C=CC=CC=3)N=2)CCN(C)CC1
|
| Solubility (In Vitro) |
DMSO: 25 mg/mL (47.57 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.43 mg/mL (2.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.43 mg/mL (2.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 14.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9027 mL | 9.5137 mL | 19.0273 mL | |
| 5 mM | 0.3805 mL | 1.9027 mL | 3.8055 mL | |
| 10 mM | 0.1903 mL | 0.9514 mL | 1.9027 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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