[CAS NO. 102676-31-3] Fadrozolehydrochloride
PRODUCTS SPECIFICATIONS [102676-31-3]
DESCRIPTION [102676-31-3]
Overview
| MDL | MFCD00866239 |
|---|---|
| Molecular Weight | 259.73 |
| Molecular Formula | C14H14ClN3 |
| SMILES | N#CC1=CC=C(C2CCCC3=CN=CN23)C=C1.Cl |
1 Publications Citing Use of MCE
Summary
Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC 50 of 6.4 nM.
IC50 & Target
IC50: 6.4 nM (aromatase) [1]
In Vitro
Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC 50 of 6.4 nM. In hamster ovarian slices, Fadrozole hydrochloride inhibits the production of estrogen with an IC 50 of 0.03 μM. The production of progesterone is inhibited with an IC 50 of 120 μM. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of Fadrozole hydrochloride [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Fadrozole hydrochloride is able to inhibit the aromatase-mediated uterine hypertrophy in immature female rats with an ED
50
of 0.03 mg/kg when given orally. In the same model, aminoglutethimide elicits the same effect with an ED
50
of 30 mg/kg when given orally
[1]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 100 mg/mL ( 385.02 mM ; Need ultrasonic and warming)
H 2 O : 100 mg/mL ( 385.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.8502 mL | 19.2508 mL | 38.5015 mL |
| 5 mM | 0.7700 mL | 3.8502 mL | 7.7003 mL |
| 10 mM | 0.3850 mL | 1.9251 mL | 3.8502 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (385.02 mM); Clear solution; Need ultrasonic
-
2.
-
3.
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
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.01 mM); Clear solution
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.
- [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.
- [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.
Synonyms
