FADROZOLE
FADROZOLE
CAS: 102676-47-1
Molecular Formula: C14H13N3
FADROZOLE - Names and Identifiers
FADROZOLE - Physico-chemical Properties
| Molecular Formula | C14H13N3 |
| Molar Mass | 223.27 |
| Density | 1.20 |
| Melting Point | 0°C |
| Boling Point | 0°C |
| Flash Point | 0°C |
| pKa | 7.16±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Physical and Chemical Properties | Melting point 117~118 ℃. Fadrazole hydrochloride (Fadrozole Hydrochloride):C14H13N3?HCl. [102676-96-0]. Crystallized from isopropanol, melting point 231-233 ℃. Soluble in water. |
| In vitro study | Fadrozole hydrochloride is a very potent inhibitor of both human placental and rat ovarian aromatase. 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. . |
| In vivo study | Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced 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. 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 dta mas in female rats, and reduces the of spontaneous hcu ar tumours in male and female rats. Administration of fadrozole in male and female mice suppresses the production of 17b-estradiol, accompanied 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 treatment returns these levels to baseline values. |
FADROZOLE - Risk and Safety
| Risk Codes | 20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. |
| Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. |
| UN IDs | 3439 |
FADROZOLE - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.479 ml | 22.394 ml | 44.788 ml |
| 5 mM | 0.896 ml | 4.479 ml | 8.958 ml |
| 10 mM | 0.448 ml | 2.239 ml | 4.479 ml |
| 5 mM | 0.09 ml | 0.448 ml | 0.896 ml |
Last Update：2024-01-02 23:10:35
FADROZOLE - Reference Information
| biological activity | Fadrozole (CGS16949A) is an effective and selective aromatase inhibitor with IC50 of 4.5 nM, which is more selective to aromatase than other cytochrome P450 enzymes. |
| target | TargetValue Aromatase () 4.5 nM |
| Target | Value |
| Aromatase () | 4.5 nM |
| in vitro study | Fadrozole hydrochloride is a very potent inhibitor of both human placental and rat ovarian aromatase. In hamster ovarian slices, fadrozole hydrochloride inhibits the production of estrogen with an IC 50 of 0.03 μ m. the production of progesterone is inhibited with an IC 50 of 120 μ m. Synthesis of other cytochrome P-450 dependent steroids can be suppressed to various degrees with higher doses of fadrozole hydrochloride .. |
| in vivo study | Fadrozole hydrochloride is able to inhibit the aromatase-mediated androstenedione-induced 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. 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 dta mas in female rats, and reduces the of spontaneous hcu ar tumours in male and female rats. Administration of fadrozole in male and female mice suppresses the production of 17b-estradiol, accompanied 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 tests of infected male mice. Fadrozole treatment returns these levels to baseline values. |
| chemical properties | melting point 117~118 ℃. Fadrazole hydrochloride (Fadrozole Hydrochloride):C14H13N3?HCl. [102676-96-0]. Crystallized from isopropanol, melting point 231-233 ℃. Soluble in water. |
| use | aromatase inhibitor. For the treatment of breast cancer. |
| Production method | The corresponding carboxylate is obtained by ammoniolysis by passing ammonia gas in dichloroethane in the presence of concentrated sulfuric acid. |
| EPA chemical information | Information provided by: ofmpub.epa.gov (external link) |
Last Update：2024-04-10 22:29:15
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