D4-abiraterone
Based on 1 Customer Validation
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
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- Reinheit: 99.85%
- CAS. Nr.: 154229-21-7
- Formel: C24H29NO
- Molecular Weight:347.50
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Speicherung:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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Biologische Aktivität
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CYP17 |
D4-abiraterone (10 mM) nearly completely blocks conversion from D4-androstenedione (AD) to 5α-androstanedione and other 5α-reduced androgens. The affinity of D4-abiraterone for mutant (expressed in LNCaP, half-maximum inhibitory concentration (IC50=5.3 nM)) and wild type (expressed in LAPC4, IC50=7.9 nM) androgen receptor (AR) is greater than that of Abiraterone (IC50=418 and >500 nM, respectively). Compare with Abiraterone, D4-abiraterone clearly better suppresses PSA, TMPRSS2 and FKBP5 expression in LNCAP, LAPC4 and C4-2 cell lines. D4-abiraterone also inhibits AR target gene expression in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 154229-21-7
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Appearance Solid
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Molecular Weight 347.50
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Formel C24H29NO
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Color White to off-white
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SMILES
C[C@@]12C(C3=CC=CN=C3)=CC[C@@]1([H])[C@]4([H])CCC5=CC(CC[C@]5(C)[C@@]4([H])CC2)=O
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Synonyms
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Lösungsmittel & Löslichkeit
DMSO : 10 mg/mL (28.78 mM; ultrasonic and warming and heat to 60°C; 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 1 mg/mL (2.88 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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: ≥ 1 mg/mL (2.88 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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.
Protokoll
To test D4-abiraterone (D4A) as an inhibitor of 3βHSD, enzyme assays are performed. Briefly, incubations are prepared with recombinant human 3βHSD1 or 3βHSD2 (in yeast microsomes, 45 or 2.5 μg protein per incubation, respectively), D4-abiraterone (5 to 20 μM) or ethanol vehicle in 0.5 mL of potassium phosphate buffer (pH 7.4). After a pre-incubation at 37°C for 1 to 3 min, NAD+ (1 mM) is added, and the incubation is conducted at 37°C for 20 min. The reaction is stopped by addition of 1 mL ethyl acetate:isooctane (1:1), and the steroids are then extracted into the organic phase and dried. The steroids in the dried extracts are resolved by HPLC and quantitated by in-line scintillation counting[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Cells are cultured in serum-free medium for 48 h and then treated with the indicated concentrations of D4-abiraterone (D4A) for 30 min. Cells are washed with 1×PBS four times and 0.9% NaCl solution twice before lysis with RIPA buffer. Intracellular radioactivity is measured with a liquid scintillation counter and normalized to the protein concentration as detected with a Multilabel counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male NSG mice, 6 to 8 weeks of age are used in this study. Mice are surgically orchiectomized and implanted with a 5 mg 90-day sustained-release dehydroepiandrosterone (DHEA) pellet to mimic castration-resistant prostate cancer (CRPC) in the context of human adrenal physiology. Two days later, 107 VCaP or C4-2 cells are injected subcutaneously with matrigel. Once tumours reach 300mm3, mice are arbitrarily (but not strictly randomized) assigned to vehicle (n=9 or 10 mice for VCaP and C4-2 respectively), D4-abiraterone (D4A) (n=10 mice for both cell lines) treatment groups. D4-abiraterone (0.5 mmol per kg per day in 0.1 mL 5% benzyl alcohol and 95% safflower oil solution) is administered via 5 mL per kg intraperitoneal injection every day for up to 15 days. Control groups are administered 0.1 mL 5% benzyl alcohol and 95% safflower oil solution via intraperitoneal injection every day. Tumour volume is measured daily, and time to increase in tumour volume by 20% is determined. Mice are killed at treatment day 15 or when the tumour size is twofold greater than baseline[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
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- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
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Handling Instructions (2659 KB)
Verweise
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 (stored under nitrogen). 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 | 2.8777 mL | 14.3884 mL | 28.7768 mL | 71.9420 mL |
| 5 mM | 0.5755 mL | 2.8777 mL | 5.7554 mL | 14.3884 mL | |
| 10 mM | 0.2878 mL | 1.4388 mL | 2.8777 mL | 7.1942 mL | |
| 15 mM | 0.1918 mL | 0.9592 mL | 1.9185 mL | 4.7961 mL | |
| 20 mM | 0.1439 mL | 0.7194 mL | 1.4388 mL | 3.5971 mL | |
| 25 mM | 0.1151 mL | 0.5755 mL | 1.1511 mL | 2.8777 mL |
D4-abiraterone Related Classifications
HY-109619 Related Classifications
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