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102676-47-1

中文名稱 法倔唑
英文名稱 FADROZOLE
CAS 102676-47-1
分子式 C14H13N3
分子量 223.27
MOL 文件 102676-47-1.mol
更新日期 2024/10/10 10:51:08
102676-47-1 結(jié)構(gòu)式 102676-47-1 結(jié)構(gòu)式

基本信息

中文別名
法倔唑
AROMATASE抑制劑(FADROZOLE)
4-(5,6,7,8-四氫咪唑[1,5-A]吡啶-5-基)苯腈
4-(5,6,7,8-四氫咪唑并[1,5-A]吡啶-5-基)苯腈
4-(5,6,7,8-四氫咪唑并[1,5-Α]吡啶-5-基)苯腈
4-(5,6,7,8-四氫咪唑并[1,5-A]吡啶-5-基)苯甲腈
英文別名
Afema
FAD286
CS-2710
FAD 286)
CGS-16949
FADROZOLE
CGS-169494
FADROZOLE USP/EP/BP
Fadrozole (CGS 16949A
Fadrozole Hydrochloride Hydrate
所屬類別
藥物: 抗腫瘤藥: 其它抗腫瘤藥物

物理化學性質(zhì)

外觀性狀熔點117~118℃。
鹽酸法屈唑(Fadrozole Hydrochloride):C14H13N3?HCl。[102676-96-0]。從異丙醇結(jié)晶,熔點231--233℃。溶于水。
熔點0°C
沸點0°C
密度1.20
閃點0°C
儲存條件2-8°C
溶解度DMSO : ≥ 100 mg/mL (447.89 mM)
酸度系數(shù)(pKa)7.16±0.40(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictogramsGHS hazard pictograms
GHS06,GHS08
警示詞危險
危險性描述H301-H361
防范說明P281-P301+P310
危險類別碼20/21/22
安全說明22-24/25
危險品運輸編號3439

應用領域

用途1
芳香酶抑制劑。用于治療乳腺癌。

制備方法

方法1
由相應的羧酸化物在二氯乙烷中,濃硫酸存在下,通入氨氣進行氨解得到。

上下游產(chǎn)品信息

上游原料
濃硫酸
法倔唑價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-14247A法倔唑
Fadrozole
102676-47-15mg660元
2024/11/08HY-14247A法倔唑
Fadrozole
102676-47-110mM * 1mLin DMSO726元
2024/11/08HY-14247A法倔唑
Fadrozole
102676-47-110mg880元

常見問題列表

生物活性
Fadrozole (CGS16949A)是一種有效的、選擇性aromatase抑制劑,IC50為4.5 nM, 對aromatase比對其他細胞色素P450酶更有選擇性。
靶點
TargetValue
Aromatase
()
4.5 nM
體外研究

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. .

體內(nèi)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.

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