ENMD-1198
Based on 1 Customer Validation
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
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- Pureza: 98.48%
- No. CAS: 864668-87-1
- Fòrmula: C20H25NO2
- Peso molecular:311.42
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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STAT3 |
HIF-1α |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
0.13 μM
Compound: 9d
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Antiangiogenic activity against HUVEC assessed as growth inhibition after 48 hrs by WST1 assay
Antiangiogenic activity against HUVEC assessed as growth inhibition after 48 hrs by WST1 assay
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[PMID: 19782564] |
| MDA-MB-231 | IC50 |
0.2 μM
Compound: 9d
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Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST1 assay
Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by WST1 assay
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[PMID: 19782564] |
ENMD-1198 (0-5 μM; 24 hours) leads to a significant dose-dependent inhibition of HCC cell growth with IC50s of 2.5 μM for HUH-7 and HepG2 cells, respectively[3].
ENMD-1198 (2.5 μM; 16 hours) abrogates EGF-induced phosphorylation of Akt (HUH-7), FAK (HUH-7), p44/42 MAPK (HepG2), and STAT3 (HUH-7, HepG2)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUH-7 and HepG2 cells
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Concentration:0-5 μM
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Incubation Time:24 hours
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Result:Led to a significant dose-dependent inhibition of HCC cell growth.
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Cell Line:HUH-7 and HepG2 cells
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Concentration:2.5 μM
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Incubation Time:16 hours
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Result:Abrogated EGF-induced phosphorylation of Akt (HUH-7), FAK (HUH-7), p44/42 MAPK (HepG2), and STAT3 (HUH-7, HepG2).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight-week-old male athymic nude mice (BALB/c nu/nu) (xenografted hepatocellular tumors)[3]
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Dosage:200 mg/kg
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Administration:P.o.; daily from day 7 to day 19
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Result:Led to a significant growth inhibition of xenografted hepatocellular tumors.
Chemical Information
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No. CAS 864668-87-1
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Appearance Solid
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Peso molecular 311.42
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Fòrmula C20H25NO2
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Color White to yellow
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SMILES
C[C@@]12C=CC[C@@]1([H])[C@]3([H])CCC4=C(C=C(OC)C(C(N)=O)=C4)[C@@]3([H])CC2
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Synonyms
IRC-110160
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (321.11 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (8.03 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.03 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Pasquier E, et al. ENMD-1198, a new analogue of 2-methoxyestradiol, displays both antiangiogenic and vascular-disrupting properties. Mol Cancer Ther. 2010 May;9(5):1408-18. [Content Brief]
[2]. Snoeks TJ, et al. 2-methoxyestradiol analogue ENMD-1198 reduces breast cancer-induced osteolysis and tumor burden both in vitro and in vivo. Mol Cancer Ther. 2011 May;10(5):874-82. [Content Brief]
[3]. Moser C, et al. ENMD-1198, a novel tubulin-binding agent reduces HIF-1alpha and STAT3 activity in human hepatocellular carcinoma(HCC) cells, and inhibits growth and vascularization in vivo. BMC Cancer. 2008 Jul 23;8:206. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2111 mL | 16.0555 mL | 32.1110 mL | 80.2774 mL |
| 5 mM | 0.6422 mL | 3.2111 mL | 6.4222 mL | 16.0555 mL | |
| 10 mM | 0.3211 mL | 1.6055 mL | 3.2111 mL | 8.0277 mL | |
| 15 mM | 0.2141 mL | 1.0704 mL | 2.1407 mL | 5.3518 mL | |
| 20 mM | 0.1606 mL | 0.8028 mL | 1.6055 mL | 4.0139 mL | |
| 25 mM | 0.1284 mL | 0.6422 mL | 1.2844 mL | 3.2111 mL | |
| 30 mM | 0.1070 mL | 0.5352 mL | 1.0704 mL | 2.6759 mL | |
| 40 mM | 0.0803 mL | 0.4014 mL | 0.8028 mL | 2.0069 mL | |
| 50 mM | 0.0642 mL | 0.3211 mL | 0.6422 mL | 1.6055 mL | |
| 60 mM | 0.0535 mL | 0.2676 mL | 0.5352 mL | 1.3380 mL | |
| 80 mM | 0.0401 mL | 0.2007 mL | 0.4014 mL | 1.0035 mL | |
| 100 mM | 0.0321 mL | 0.1606 mL | 0.3211 mL | 0.8028 mL |
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