Rezvilutamide
Based on 1 Customer Validation
Rezvilutamide (SHR3680) is an orally active androgen receptor antagonist. Rezvilutamide (SHR3680) is used for the study of prostate cancer.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 1572045-62-5
- Formula: C22H20F3N3O4S
- Molecular Weight:479.47
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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
Rezvilutamide inhibits the nuclear translocation, transcriptional activity, overexpression and secretion of prostate-specific antigen of androgen receptor in prostate cancer cells, exhibits an inducing effect on CYP3A4 and CYP2B6[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1572045-62-5
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Appearance Solid
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Molecular Weight 479.47
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Formula C22H20F3N3O4S
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Color White to off-white
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SMILES
S=C(N(C(C=C1)=CC=C1OC[C@@H](O)CO)C(C)2C)N(C(C=C3)=CC(C(F)(F)F)=C3C#N)C2=O
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Synonyms
SHR3680
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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 : 100 mg/mL (208.56 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: ≥ 2.5 mg/mL (5.21 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 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 (5.21 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.
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
[2]. Veronica Mollica, et al. Molecular Mechanisms Related to Hormone Inhibition Resistance in Prostate Cancer. Cells. 2019 Jan 11;8(1):43. [Content Brief]
[3]. Dai T, et al., A single-centre, open-label, single-arm, fixed-sequence pharmacokinetic study of SHR3680 on repaglinide and bupropion in prostate cancer patients. Br J Clin Pharmacol. 2023 Feb;89(2):874-886. [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 | 2.0856 mL | 10.4282 mL | 20.8564 mL | 52.1409 mL |
| 5 mM | 0.4171 mL | 2.0856 mL | 4.1713 mL | 10.4282 mL | |
| 10 mM | 0.2086 mL | 1.0428 mL | 2.0856 mL | 5.2141 mL | |
| 15 mM | 0.1390 mL | 0.6952 mL | 1.3904 mL | 3.4761 mL | |
| 20 mM | 0.1043 mL | 0.5214 mL | 1.0428 mL | 2.6070 mL | |
| 25 mM | 0.0834 mL | 0.4171 mL | 0.8343 mL | 2.0856 mL | |
| 30 mM | 0.0695 mL | 0.3476 mL | 0.6952 mL | 1.7380 mL | |
| 40 mM | 0.0521 mL | 0.2607 mL | 0.5214 mL | 1.3035 mL | |
| 50 mM | 0.0417 mL | 0.2086 mL | 0.4171 mL | 1.0428 mL | |
| 60 mM | 0.0348 mL | 0.1738 mL | 0.3476 mL | 0.8690 mL | |
| 80 mM | 0.0261 mL | 0.1304 mL | 0.2607 mL | 0.6518 mL | |
| 100 mM | 0.0209 mL | 0.1043 mL | 0.2086 mL | 0.5214 mL |