Fadrozole (hydrochloride) (Synonyms: CGS 16949A) |
| Katalog-Nr.GC18301 |
Fadrozol (Hydrochlorid) (CGS 16949A) ist ein potenter, selektiver und nichtsteroidaler Aromatasehemmer mit einem IC50 von 6,4 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 102676-31-3
Sample solution is provided at 25 µL, 10mM.
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Fadrozole is a non-steroidal aromatase inhibitor (IC50s = 5 and 1.4 nM for human placental and rat ovarian microsomal aromatase, respectively). It selectively inhibits estrogen over progesterone production induced by luteinizing hormone (LH) in hamster ovarian tissue as well as corticosterone and aldosterone production induced by adrenocorticotropic hormone in rat adrenal tissue (IC50s = 0.03, 160, 100, and 1 μM, respectively). It also decreases ovarian estrogen levels in rats when administered at a dose of 0.26 mg/kg. Fadrozole inhibits conversion of cholesterol to 27-hydroxycholesterol by the cytochrome P450 (CYP) isomer 27A1 (Ki = 4.6 μM). It inhibits growth of androstenedione-stimulated mammary D2 cells implanted into thoracic mammary fat pads of mice by 95% when administered at a dose of 0.5 mg per animal per day.
References:
[1]. Bhatnagar, A.S., H?usler, A., Schieweck, K., et al. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor J. Steroid Biochem. Mol. Biol. 37(6), 1021-1027 (1990).
[2]. Steele, R.E., Mellor, L.B., Sawyer, W.K., et al. In vitro and in vivo studies demonstrating potent and selective estrogen inhibition with the nonsteroidal aromatase inhibitor CGS 16949A Steroids 50(1-3), 147-161 (1987).
[3]. Mast, N., Lin, J.B., and Pikuleva, I.A. Marketed drugs can inhibit cytochrome P450 27A1, a potential new target for breast cancer adjuvant therapy Mol. Pharmacol. 88(3), 428-436 (2015).
[4]. Tekmal, R.R., and Durgam, V.R. A novel in vitro and in vivo breast cancer model for testing inhibitors of estrogen biosynthesis and its action using mammary tumor cells with an activated int-5/aromatase gene Cancer Lett. 118(1), 21-28 (1997).
Animal experiment: | 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]. |
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. | |
| Cas No. | 102676-31-3 | SDF | |
| Überlieferungen | CGS 16949A | ||
| Chemical Name | 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)-benzonitrile, monohydrochloride | ||
| Canonical SMILES | N#CC(C=C1)=CC=C1C(CCC2)N3C2=CN=C3.Cl | ||
| Formula | C14H13N3.HCl | M.Wt | 259.7 |
| Löslichkeit | DMF: 5 mg/ml,DMSO: 10 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml,Ethanol: 2 mg/ml | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.8506 mL | 19.253 mL | 38.506 mL |
| 5 mM | 0.7701 mL | 3.8506 mL | 7.7012 mL |
| 10 mM | 0.3851 mL | 1.9253 mL | 3.8506 mL |
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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: >99.00%
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Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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