Ar-V7-IN-1
Based on 1 Customer Validation
Ar-V7-IN-1 is a potent inhibitor of Ar-V7. Ar-V7-IN-1 inhibits the transcriptional activity of androgen receptor (AR) and the secretion of prostate-specific antigen (PSA) with an eGFP IC50 of 1232 nM and the PSA IC50 of 1391 μM. Ar-V7-IN-1 has the potential for the research of various indications, in particular cancers such as prostate cancer.
For research use only. We do not sell to patients.
- Purity: 98.02%
- CAS No.: 2230880-25-6
- Formula: C10H10Br2N4OS
- Molecular Weight:394.09
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
<0.5 μM
Compound: 128
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Antiproliferative activity against human LNCaP cells
Antiproliferative activity against human LNCaP cells
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[PMID: 35786895] |
| LNCaP | IC50 |
0.1 μM
Compound: 25
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Inhibition of androgen receptor transcriptional activity in human LNCaP cells after 3 days by eGFP assay
Inhibition of androgen receptor transcriptional activity in human LNCaP cells after 3 days by eGFP assay
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[PMID: 25062331] |
| LNCaP | IC50 |
0.17 μM
Compound: 25
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Inhibition of androgen receptor in human LNCaP cells assessed as inhibition of prostate-specific antigen secretion into media after 3 days
Inhibition of androgen receptor in human LNCaP cells assessed as inhibition of prostate-specific antigen secretion into media after 3 days
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[PMID: 25062331] |
| MR49F | IC50 |
<0.5 μM
Compound: 128
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Antiproliferative activity against human MR49F cells
Antiproliferative activity against human MR49F cells
|
[PMID: 35786895] |
Ar-V7-IN-1 (Compound 43) exhibits human microsomal stability with a Clint of 165 μL/min/mg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2230880-25-6
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Appearance Solid
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Molecular Weight 394.09
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Formula C10H10Br2N4OS
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Color White to off-white
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SMILES
BrC1=C(Br)N(C2=CSC(N3CCOCC3)=N2)C=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 83.33 mg/mL (211.45 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)
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: ≥ 2.08 mg/mL (5.28 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 | 2.5375 mL | 12.6875 mL | 25.3749 mL | 63.4373 mL |
| 5 mM | 0.5075 mL | 2.5375 mL | 5.0750 mL | 12.6875 mL | |
| 10 mM | 0.2537 mL | 1.2687 mL | 2.5375 mL | 6.3437 mL | |
| 15 mM | 0.1692 mL | 0.8458 mL | 1.6917 mL | 4.2292 mL | |
| 20 mM | 0.1269 mL | 0.6344 mL | 1.2687 mL | 3.1719 mL | |
| 25 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL | 2.5375 mL | |
| 30 mM | 0.0846 mL | 0.4229 mL | 0.8458 mL | 2.1146 mL | |
| 40 mM | 0.0634 mL | 0.3172 mL | 0.6344 mL | 1.5859 mL | |
| 50 mM | 0.0507 mL | 0.2537 mL | 0.5075 mL | 1.2687 mL | |
| 60 mM | 0.0423 mL | 0.2115 mL | 0.4229 mL | 1.0573 mL | |
| 80 mM | 0.0317 mL | 0.1586 mL | 0.3172 mL | 0.7930 mL | |
| 100 mM | 0.0254 mL | 0.1269 mL | 0.2537 mL | 0.6344 mL |