Fadrozole hydrochloride
Based on 3 publication(s) in Google Scholar
Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
For research use only. We do not sell to patients.
- Purity: 99.91%
- CAS No.: 102676-31-3
- Formula: C14H14ClN3
- Molecular Weight:259.73
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Fadrozole hydrochloride
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Biological Activity
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Aromatase |
Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM. In hamster ovarian slices, Fadrozole hydrochloride inhibits the production of estrogen with an IC50 of 0.03 μM. The production of progesterone is inhibited with an IC50 of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of Fadrozole hydrochloride[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Fadrozole hydrochloride prevents the development of both benign and malignant spontaneus mammary neoplasns in female Sprague-Dawley rats. It also slows the spontaneous development of ptuitary pars distalis adenomas in female rats, and reduces the incidence of spontaneous hepatocellular tumours in male and female rats[2].
Administration of Fadrozole hydrochloride in male and female mice accompanies with a 70% reduction in parasite burden. This protective effect is associated in male mice with a recovery of the specific cellular immune response. Interleukin-6 (IL-6) serum levels, and its production by splenocytes, is augmented by 80%, together with a 10-fold increase in its expression in testes of infected male mice. Fadrozole hydrochloride treatment returns these levels to baseline values[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 102676-31-3
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Appearance Solid
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Molecular Weight 259.73
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Formula C14H14ClN3
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Color White to off-white
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SMILES
N#CC1=CC=C(C2CCCC3=CN=CN23)C=C1.Cl
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Synonyms
CGS 16949A; (Rac)-FAD286 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Ecotoxicol Environ Saf
Effect of bisphenol A on craniofacial cartilage development in zebrafish (Danio rerio) embryos: A morphological study. [Abstract]2021 Apr 1:212:111991. PMID: 33548570 -
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Dis Model Mech
Sex hormone receptors, calcium-binding protein and Yap1 signaling regulate sex-dependent liver cell proliferation following partial hepatectomy. [Abstract]2024 Oct 1;17(10):dmm050900. PMID: 39397390
Solvent & Solubility
DMSO : 100 mg/mL (385.02 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 100 mg/mL (385.02 mM; Need ultrasonic)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (8.01 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (8.01 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 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (385.02 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
Rats: Rats are treated with daily dosing with Fadrozole hydrochloride in purified water by gavage for 2 years. There are 60 rats in each of four groups given 0, 0.05, 0.25 or 1.25 mg/kg daily. Control rats receive only water. Clinical signs are recorded weekly and the animals are examined for palpable masses every 4 weeks for the first 9 months, then every 2 weeks for the remainder of the study[2].
Mice: Fadrozole hydrochloride is administered in the form of sub-dermal long-term release pellets (20 mg/wt kg, in three-week-release pellets), starting 1 week prior to the infection, using a 10-gauge needle. Three pellets are administrated during the study. Placebo pellets are administered to another group of infected mice, in the same fashion as the inhibitor. After 1 week, mice are infected and killed 8 weeks later[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (584 KB)
- English - EN (584 KB)
- Français - FR (584 KB)
- Deutsch - DE (584 KB)
- Norwegian - NO (584 KB)
- Español - ES (584 KB)
- Swedish - SV (584 KB)
- Italian - IT (584 KB)
- Korean - KR (584 KB)
- Portuguese - PT (584 KB)
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Handling Instructions (2659 KB)
References
[1]. Browne LJ, et al. Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. J Med Chem. 1991 Feb;34(2):725-36. [Content Brief]
[2]. Gunson DE, et al. Prevention of spontaneous tumours in female rats by fadrozole hydrochloride, an aromatase inhibitor. Br J Cancer. 1995 Jul;72(1):72-5. [Content Brief]
[3]. Morales-Montor J, et al. Inhibition of p-450 aromatase prevents feminisation and induces protection during cysticercosis. Int J Parasitol. 2002 Oct;32(11):1379-87. [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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 3.8502 mL | 19.2508 mL | 38.5015 mL | 96.2538 mL |
| 5 mM | 0.7700 mL | 3.8502 mL | 7.7003 mL | 19.2508 mL | |
| 10 mM | 0.3850 mL | 1.9251 mL | 3.8502 mL | 9.6254 mL | |
| 15 mM | 0.2567 mL | 1.2834 mL | 2.5668 mL | 6.4169 mL | |
| 20 mM | 0.1925 mL | 0.9625 mL | 1.9251 mL | 4.8127 mL | |
| 25 mM | 0.1540 mL | 0.7700 mL | 1.5401 mL | 3.8502 mL | |
| 30 mM | 0.1283 mL | 0.6417 mL | 1.2834 mL | 3.2085 mL | |
| 40 mM | 0.0963 mL | 0.4813 mL | 0.9625 mL | 2.4063 mL | |
| 50 mM | 0.0770 mL | 0.3850 mL | 0.7700 mL | 1.9251 mL | |
| 60 mM | 0.0642 mL | 0.3208 mL | 0.6417 mL | 1.6042 mL | |
| 80 mM | 0.0481 mL | 0.2406 mL | 0.4813 mL | 1.2032 mL | |
| 100 mM | 0.0385 mL | 0.1925 mL | 0.3850 mL | 0.9625 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Fadrozole hydrochloride Related Classifications
HY-14247 Related Classifications
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