| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| Targets |
MYC
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|---|---|
| ln Vitro |
En4 inhibits MYC transcriptional activity, downregulates numerous MYC transcriptional targets, directly targets MYC in cells, decreases MYC and MAX thermal stability, and hinders tumorigenesis. Treatment with EN4 significantly reduces the proliferation of 231MFP breast cancer cells in a dose- and time-dependent manner. Mammary epithelial MCF10A cells that have undergone MYC transformation are less likely to survive when exposed to EN4, but not parental MCF10A cells that are not MYC-dependent. [1]
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| ln Vivo |
In immune-deficient mice, EN4 treatment that is started after the establishment of a 231MFP breast tumor xenograft significantly slows tumor growth in vivo.[1]
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| Cell Assay |
In 6 cm dishes, 231MFP cells are plated, and they are then given DMSO vehicle or EN4 (50 μM) treatment for 24 hours. Scraping is used to collect the cells, and the Qiagen RNeasy mini kit and Qiagen DNase max kit are used to isolate the RNA and remove any DNA contamination. The KAPA mRNA Capture Kit's Oligo dT beads are used to enrich for mRNA.
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| References |
| Molecular Formula |
C25H24N2O4
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|---|---|
| Molecular Weight |
416.477
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| Exact Mass |
416.1736
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| Elemental Analysis |
C, 72.10; H, 5.81; N, 6.73; O, 15.37
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| CAS # |
1197824-15-9
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| Related CAS # |
1197824-15-9
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C2C=C(C=CC2=C1)CCOC3=C(C=CC(=C3)CN4C=CC=N4)COCC(=O)O
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| InChi Key |
BHCJZNGDYXVVII-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H24N2O4/c28-25(29)18-30-17-23-9-7-20(16-27-12-3-11-26-27)15-24(23)31-13-10-19-6-8-21-4-1-2-5-22(21)14-19/h1-9,11-12,14-15H,10,13,16-18H2,(H,28,29)
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| Chemical Name |
2-[[2-(2-naphthalen-2-ylethoxy)-4-(pyrazol-1-ylmethyl)phenyl]methoxy]acetic acid
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| Synonyms |
EN-4; EN4; EN 4; EN4 MYC inhibitor
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 83~125 mg/mL (199.3~300.1 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.99 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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: 2.08 mg/mL (4.99 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4011 mL | 12.0054 mL | 24.0108 mL | |
| 5 mM | 0.4802 mL | 2.4011 mL | 4.8022 mL | |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.4011 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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