|4-(5,6,7,8-四氢咪唑并[1,5-a]吡啶-5-基)苯腈盐酸盐|CsnPharm

CAS No.: 102676-31-3

4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile hydrochloride Catalog No. CSN19726

Synonyms: CGS 16949A;(Rac)-FAD286 hydrochloride;FAD286

Fadrozole HCl specifically inhibits aromatase, blocking the aromatization of androstenedione and testosterone into estrone and estradiol, respectively.

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技术信息

生物活性

描述The aromatase inhibitors have proven to be efficacious in the treatment of estrogen-dependent diseases. Fadrozole HCl is a potent, selective, orally active, nonsteroidal inhibitor of aromatase with an IC50 value of 6.4nM. It is approximately 1000 times more selective than aminoglutethimide in inhibiting aromatase. Fadrozole HCl inhibited the production of estrogen with an IC50 value of 0.03μM in hamster ovarian slices. In immature female rats, oral administration of fadrozole HCl inhibited aromatase-mediated androstenedione-induced uterine hypertrophy with an EC50 value of 0.03mg/kg. In female rats bearing DMBA-induced mammary tumors, oral administration of fadrozole HCl almost completely suppressed the appearance of new tumors and inhibited the growth of palpable tumors with an ED50 value of 0.1mg/kg/day. The maximal anti-tumor effect was observed at a dosage of 2mg/kg/day^[3].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00247663	Postmenopausal Women With Adva... more >>nced Breast Cancer Collapse <<	Phase 2	Completed	-	Japan ... more >> Novartis Investigative Site Kashiwa, Chiba, Japan, 277-8577 Novartis Investigative Site Amagasaki, Hyogo, Japan, 660-8511 Novartis Investigative Site Hamamatsu, Shizuoka, Japan, 430-8558 Novartis Investigative Site Chuo-Ku, Tokyo, Japan, 104-0045 Novartis Investigative Site Cyuo-ku, Tokyo, Japan, 104-8560 Novartis Investigative Site Shinjuku-ku, Tokyo, Japan, 160-8582 Novartis Investigative Site Fukuoka, Japan, 811-4395 Novartis Investigative Site Kumamoto, Japan, 862-0909 Novartis Investigative Site Nigata, Japan, 951-8566 Novartis Investigative Site Saitama, Japan, 338-8553 Collapse <<
NCT03279289	Metastatic Colorectal Cancer	Phase 2	Recruiting	July 2021	Spain ... more >> Spanish Cooperative Group for Digestive Tumour Therapy (TTD) Recruiting Madrid, Spain, 28046 Contact: Inmaculada Ruiz de Mena, PhD 0034 91 378 82 75 ttd@ttdgroup.org Collapse <<

参考文献

[1] Zhang D, Popesku JT, et al. Profiling neuroendocrine gene expression changes following fadrozole-induced estrogen decline in the female goldfish. Physiol Genomics. 2009 Aug 7;38(3):351-61.
[2] Luzio A, Matos M, et al. Disruption of apoptosis pathways involved in zebrafish gonad differentiation by 17α-ethinylestradiol and fadrozole exposures. Aquat Toxicol. 2016 Aug;177:269-84
[3] Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A. 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8501 mL
- 19.2505 mL
- 38.5009 mL
- 5 mM
- 0.7700 mL
- 3.8501 mL
- 7.7002 mL
- 10 mM
- 0.3850 mL
- 1.9250 mL
- 3.8501 mL

技术信息

CAS号

102676-31-3

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H14ClN3

运输

蓝冰

分子量

259.73

别名

CGS 16949A;(Rac)-FAD286 hydrochloride;FAD286;Fadrozole (hydrochloride);Fadrozole HCl;Fadrozole

溶解度

DMSO	95.0 mg/mL (365.8 mM) warming
Water	100.0 mg/mL (385.0 mM) warming

动物实验配方

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4-(5,6,7,8-Tetrahydroimidazo[1,5-a]pyridin-5-yl)benzonitrile hydrochloride Catalog No. CSN19726

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