AGN194204
Based on 1 Customer Validation
AGN194204 (IRX4204) is an orally active and selective RXR agonist with Kd values 0.4 nM, 3.6 nM and 3.8 nM and EC50s of 0.2 nM, 0.8 nM and 0.08 nM for RXRα, RXRβ and RXRγ, respectively. AGN194204 is inactive against RAR. AGN194204 has anti-inflammatory and anticarcinogenic actions.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.79%
- No. CAS: 220619-73-8
- Fòrmula: C24H32O2
- Peso molecular:352.51
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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TTNPBApoptosis Inducer
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | EC50 |
0.08 nM
Compound: 2
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Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR gamma
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[PMID: 11428923] |
| CV-1 | EC50 |
0.2 nM
Compound: 2
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Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR alpha
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[PMID: 11428923] |
| CV-1 | EC50 |
0.8 nM
Compound: 2
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Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta
Transcriptional activation in CV-1 cells expressing retinoid X receptor RXR beta
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[PMID: 11428923] |
| CV-1 | IC50 |
6 nM
Compound: 2
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In vitro antagonist activity against RXR alpha in CV-1 cells
In vitro antagonist activity against RXR alpha in CV-1 cells
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[PMID: 14592510] |
In Vitro
AGN194204 (NRX194204; 0-100 nM; 24 hours; E, RAW cells) treatment blocks the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells[1].
AGN194204 (NRX194204; 1 μM; 72 hours; SK-BR-3 human breast cancer cells) treatment induces apoptosis in breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-BR-3 human breast cancer cells
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Concentration:1 μM
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Incubation Time:72 hours
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Result:Induced apoptosis in lung and breast cancer cells.
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Cell Line:E, RAW cells
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Concentration:0 nM, 1 nM, 10 nM and 100 nM
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Incubation Time:24 hours
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Result:Blocked the ability of lipopolysaccharide and tumor necrosis factor-α to induce the release of nitric oxide and interleukin 6 and the degradation of IKBα in RAW264.7 macrophage-like cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female A/J mice with vinyl carbamate[1]
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Dosage:30 mg/kg, 60 mg/kg
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Administration:Oral administration; daily; for 15 weeks
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Result:Significantly reduced the number and size of tumors on the surface of the lungs and reduced the total tumor volume per slide by 64% to 81% compared with the control group.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 220619-73-8
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Appearance Solid
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Peso molecular 352.51
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Fòrmula C24H32O2
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Color White to off-white
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SMILES
O=C(O)/C=C(C)/C=C/[C@H]1[C@](C2=CC=C3C(C)(C)CCC(C)(C)C3=C2)(C)C1
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Synonyms
IRX4204; NRX194204; VTP 194204
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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
In Vitro:
DMSO : 100 mg/mL (283.68 mM; Need ultrasonic; 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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 (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liby K, et al. A new rexinoid, NRX194204, prevents carcinogenesis in both the lung and mammary gland. Clin Cancer Res. 2007 Oct 15;13(20):6237-43. [Content Brief]
[2]. Vuligonda V, et al. Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes. J Med Chem. 2001 Jul 5;44(14):2298-303. [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 | 2.8368 mL | 14.1840 mL | 28.3680 mL | 70.9200 mL |
| 5 mM | 0.5674 mL | 2.8368 mL | 5.6736 mL | 14.1840 mL | |
| 10 mM | 0.2837 mL | 1.4184 mL | 2.8368 mL | 7.0920 mL | |
| 15 mM | 0.1891 mL | 0.9456 mL | 1.8912 mL | 4.7280 mL | |
| 20 mM | 0.1418 mL | 0.7092 mL | 1.4184 mL | 3.5460 mL | |
| 25 mM | 0.1135 mL | 0.5674 mL | 1.1347 mL | 2.8368 mL | |
| 30 mM | 0.0946 mL | 0.4728 mL | 0.9456 mL | 2.3640 mL | |
| 40 mM | 0.0709 mL | 0.3546 mL | 0.7092 mL | 1.7730 mL | |
| 50 mM | 0.0567 mL | 0.2837 mL | 0.5674 mL | 1.4184 mL | |
| 60 mM | 0.0473 mL | 0.2364 mL | 0.4728 mL | 1.1820 mL | |
| 80 mM | 0.0355 mL | 0.1773 mL | 0.3546 mL | 0.8865 mL | |
| 100 mM | 0.0284 mL | 0.1418 mL | 0.2837 mL | 0.7092 mL |
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