法倔唑
中文名称:
法倔唑
中文同义词:
法倔唑;4-(5,6,7,8-四氢咪唑并[1,5-Α]吡啶-5-基)苯腈;AROMATASE抑制剂(FADROZOLE);4-(5,6,7,8-四氢咪唑并[1,5-A]吡啶-5-基)苯甲腈;4-(5,6,7,8-四氢咪唑[1,5-A]吡啶-5-基)苯腈
英文名称:
FADROZOLE
英文同义词:
FADROZOLE;4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridine-5-yl)benzonitrile;4-[(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin)-5-yl]benzonitrile;4-[[5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin]-5-yl]benzonitrile;5,6,7,8-Tetrahydro-5-(4-cyanophenyl)imidazo[1,5-a]pyridine;CGS-16949;Fadrozole Hydrochloride Hydrate;Afema
CAS号:
102676-47-1
分子式:
C14H13N3
分子量:
223.27
EINECS号:
相关类别:
细胞生物学试剂;抗肿瘤药;其它抗肿瘤药物;药物
Mol文件:
102676-47-1.mol
熔点
0°C
沸点
0°C
密度
1.20
闪点
0°C
储存条件
Sealed in dry,2-8°C
酸度系数(pKa)
7.16±0.40(Predicted)
EPA化学物质信息
Benzonitrile, 4-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-5-yl)- (102676-47-1)
生物活性
Fadrozole (CGS16949A)是一种有效的、选择性aromatase抑制剂，IC50为4.5 nM, 对aromatase比对其他细胞色素P450酶更有选择性。
靶点
Target Value
Aromatase
() 4.5 nM
Target
Value
Aromatase
()
4.5 nM
体外研究
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. .
体内研究
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.
化学性质
熔点117～118℃。
盐酸法屈唑(Fadrozole Hydrochloride)：C14H13N3?HCl。[102676-96-0]。从异丙醇结晶，熔点231--233℃。溶于水。
用途
芳香酶抑制剂。用于治疗乳腺癌。
生产方法
由相应的羧酸化物在二氯乙烷中，浓硫酸存在下，通入氨气进行氨解得到。
危险类别码
20/21/22
安全说明
22-24/25
危险品运输编号
3439
