Ralaniten
Based on 1 Customer Validation
Ralaniten (EPI-002) is a potent and orally active antagonist of the androgen receptor-N-terminal domain (AR-NTD). Ralaniten inhibits AR transcriptional activity, with IC50 of 7.4 μM. Ralaniten can be used for the research of castration-resistant prostate cancer (CRPC).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.57%
- No. CAS: 1203490-23-6
- Fòrmula: C21H27ClO5
- Peso molecular:394.89
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Actividad biológica
Descripciòn
IC50 & Target
IC50: 7.4 μM (AR-NTD)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
>30 μM
Compound: EPI-002
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Antiproliferative activity against enzalutamide-resistant human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
Antiproliferative activity against enzalutamide-resistant human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
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[PMID: 37556600] |
| CWR22R | IC50 |
40.4 μM
Compound: EPI002
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Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38512060] |
| LNCaP | IC50 |
>30 μM
Compound: EPI-002
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Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
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[PMID: 37556600] |
| VCaP | IC50 |
>30 μM
Compound: EPI-002
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Antiproliferative activity against human VCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
Antiproliferative activity against human VCaP cells assessed as reduction in cell viability incubated for 6 days by CCK-8 assay
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[PMID: 37556600] |
In Vitro
EPI-002 (5-35 μM; 2-3 days) reduces AR-dependent proliferation of LNCaP cells, and has no effect on the viability of PC3 human prostate cancer cells that do not express functional AR[1].
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Ralaniten (10-35 μM; 4 h) inhibits transactivation of the AR N-terminal domain (NTD) induced by forskolin in LNCaP cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male NOD-SCID mice bearing subcutaneous tumors were castrated
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Dosage:100 mg/kg
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Administration:P.o. twice daily for 28 days
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Result:Inhibited the growth of castration-resistant prostate cancer (CRPC) xenografts that express AR splice variants[1].
Chemical Information
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No. CAS 1203490-23-6
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Appearance Solid
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Peso molecular 394.89
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Fòrmula C21H27ClO5
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Color White to off-white
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SMILES
CC(C1=CC=C(OC[C@H](O)CCl)C=C1)(C2=CC=C(OC[C@H](O)CO)C=C2)C
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Synonyms
EPI-002
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (253.24 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 (protect from light). 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 (protect from light). 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Protocolo
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Dual Luciferin reporter gene assay
Luciferin reporter gene assay is a reporting system to detect the activity of Firefly Luciferase using luciferin as a substrate, which is often used in the research of miRNA target gene verification and promoter transcriptive activity regulation. Dual luciferase usually refers to Firefly luciferase and Renilla luciferase.
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureza y Documentación
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Ficha de datos (270 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]. Myung JK, et, al. An androgen receptor N-terminal domain antagonist for treating prostate cancer. J Clin Invest. 2013 Jul;123(7):2948-60. [Content Brief]
[2]. Yang YC, et, al. Targeting Androgen Receptor Activation Function-1 with EPI to Overcome Resistance Mechanisms in Castration-Resistant Prostate Cancer. Clin Cancer Res. 2016 Sep 1;22(17):4466-77. [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 (protect from light). 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 | 2.5324 mL | 12.6618 mL | 25.3235 mL | 63.3088 mL |
| 5 mM | 0.5065 mL | 2.5324 mL | 5.0647 mL | 12.6618 mL | |
| 10 mM | 0.2532 mL | 1.2662 mL | 2.5324 mL | 6.3309 mL | |
| 15 mM | 0.1688 mL | 0.8441 mL | 1.6882 mL | 4.2206 mL | |
| 20 mM | 0.1266 mL | 0.6331 mL | 1.2662 mL | 3.1654 mL | |
| 25 mM | 0.1013 mL | 0.5065 mL | 1.0129 mL | 2.5324 mL | |
| 30 mM | 0.0844 mL | 0.4221 mL | 0.8441 mL | 2.1103 mL | |
| 40 mM | 0.0633 mL | 0.3165 mL | 0.6331 mL | 1.5827 mL | |
| 50 mM | 0.0506 mL | 0.2532 mL | 0.5065 mL | 1.2662 mL | |
| 60 mM | 0.0422 mL | 0.2110 mL | 0.4221 mL | 1.0551 mL | |
| 80 mM | 0.0317 mL | 0.1583 mL | 0.3165 mL | 0.7914 mL | |
| 100 mM | 0.0253 mL | 0.1266 mL | 0.2532 mL | 0.6331 mL |
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