Fadrozole |
Catalog No.GC19151
One-Click Copy Product Info
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Fadrozole (CGS 16949A) is a selective, non-steroidal aromatase inhibitor with an IC50 value of 4.5μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 102676-47-1
Sample solution is provided at 25 µL, 10mM.
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Fadrozole (CGS 16949A) is a selective, non-steroidal aromatase inhibitor with an IC50 value of 4.5μM[1]. Fadrozole has been investigated as a treatment of hormone-responsive breast cancer (estrogen sensitive)[1]. Aromatase is an enzyme that plays a vital role in converting androgens (like testosterone) into estrogens (like estradiol). Fadrozole can be used to block aromatase and reduces the level of estrogens[2].
In vitro, prolactin-positive cells were extracted from male Wistar rats. By treating prolactin-positive cells with 1μM Fadrozole alone for 1, 3, 6 or 12 hours respectively, no statistically significant variations in the cellular area and proliferation rates were observed due to absent testosterone and minimal synthesized estradiol[3]. When treating cells with 1μM Fadrozole and 1μM testosterone, significantly decreased of the size of prolactin-positive cells as well as reduced percentage of proliferation rates were obtained from 3 to 12 hours treatment[3].
In vivo, Fadrozole (300μg/day) was inplantated with mini-osmotic pumps on day 14 of pregnancy Sprague–Dawley rats to reduce the level of estradiol-17 (E2)[4]. Fadrozole (1200μg; 4 days) resulted in a significant reduced E2 concentration and high level of androstenedione and testosterone in pregnant rats[4]. Fadrozole (1800μg; 6 days) led to a fourfold increased intrauterine pressure with significant smaller uterine tissue framework in pregnant rats[2,4]. Fadrozole caused fetal abnormalities in pregnant rats, where 20% of fetuses had head injuries while their weight did not differ from normal fetuses[4].
References:
[1] Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A. Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease. Journal of medicinal chemistry. 1991 Feb;34(2):725-36.
[2] Tiboni GM, Ponzano A. Fetal safety profile of aromatase inhibitors: Animal data. Reproductive Toxicology. 2016 Dec 1;66:84-92.
[3] Patil CN, Li W, Wang X. Local transformations of androgens into estradiol by aromatase P450 are involved in the regulation of prolactin and the proliferation of pituitary prolactin-positive cells. J Endocrinol. 2014;222(2):201–12. doi:10.1530/JOE-13-0579.
[4] Tamada H, Shimizu Y, Inaba T, Kawate N, Sawada T. The effects of the aromatase inhibitor fadrozole hydrochloride on fetuses and uteri in late pregnant rats. Journal of endocrinology. 2004 Feb 1;180(2):337-46.
| Cell experiment [1]: | |
Cell lines | Prolactin-positive cells |
Preparation Method | Male Wistar rats (175–200g) were killed to extract prolactin-positive cells. Prolactin-positive cells were seeded on 60 culture chamber slides at a final concertation of 2.5×105/ml cells and incubated with Dulbecco’s modified Eagle’s medium (DMEM) for 7 days. On day 4, medium was changed by fresh DMEM. On day 7, cell cultures were treated with 1μM testosterone, 1μM Fadrozole and incubated for 1, 3, 6 or 12 hours (5 chambers per treatment). After treatment, the chambers were washed with Dubelcco’s sterile PBS, and cells were fixed in Somogy’s solution for 1 hour, followed by rinsing in PBS. |
Reaction Conditions | 1μM testosterone, 1μM Fadrozole; 1, 3, 6 or 12 hours |
Applications | Fadrozole alone did not affect prolactin-positive cells. Combination of Fadrozole and testosterone significantly decreases prolactin-positive cells sizes and proliferation rates. |
| Animal experiment [2]: | |
Animal models | Sprague–Dawley female rats |
Preparation Method | Female rats (180-300g) were mated when 60-120 days old. On day 14 of pregnancy rats were divided into three groups. Group 1 (Fad) rats were implanted s.c. with mini-osmotic pumps containing Fadrozole (300μg/day). Group 2 (control) rats were implanted s.c. with mini-osmotic pumps containing saline. Group 3 (Fad+E2) rats were implanted s.c. with mini-osmotic pumps containing Fadrozole (300μg/day) and estradiol-17 (E2) (0.2μg/day, E2 was dissolved in 0.2ml sesame oil). On day 17 of pregnancy, blood samples were collected from the abdominal aorta of rats in all 3 groups. On day 20 of pregnancy, all 3 groups rats underwent laparotomy under ether anesthesia. |
Dosage form | Fadrozole: 300μg/day for 6 days; estradiol-17: 0.2μg/day for 6 days |
Applications | Fadrozole treatment significantly reduced E2 concentration, and led to a fourfold increased intrauterine pressure with smaller uterine tissue framework in pregnant rats. Fadrozole caused fetal abnormalities in pregnant rats, but their weight did not differ from normal fetuses. The combination treatment of Fadrozole and E2 had similar effect as control groups, indicating that exogenously supplied E2 could compensate for the loss of endogenous E2. |
References: | |
| Cas No. | 102676-47-1 | SDF | |
| Canonical SMILES | N#CC1=CC=C(C2CCCC3=CN=CN23)C=C1 | ||
| Formula | C14H13N3 | M.Wt | 223.27 |
| Solubility | DMSO : ≥ 100 mg/mL (447.89 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4789 mL | 22.3944 mL | 44.7888 mL |
| 5 mM | 895.8 μL | 4.4789 mL | 8.9578 mL |
| 10 mM | 447.9 μL | 2.2394 mL | 4.4789 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)