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Fadrozole

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Chemical Structure| 102676-47-1 同义名 : CGS 16949A free base;(Rac)-FAD286;CGS16949A
CAS号 : 102676-47-1
货号 : A428094
分子式 : C14H13N3
纯度 : 95%
分子量 : 223.273
MDL号 : MFCD02313480
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(470.28 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Estrogen is a sex hormone implicated in the progression of many diseases. Aromatase is a key enzyme responsible for the biosynthesis of estrogen. Fadrozole is a potent, selective, nonsteroidal inhibitor of aromatase that can be used for the treatment of estrogen-dependent diseases. Fadrozole inhibits aromatase at an IC50 value of 6.4nM. Fadrozole also inhibited the production of estrogen in hamster ovarian slices with an IC50 of 0.03μM. In immature female rats, orally administration of fadrozole inhibited aromatase-mediated, androstenedione-induced uterine hypertrophy with an ED50 value of 0.03mg/kg[2].
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... 展开 >>nced Breast Cancer 收起 << Phase 2 Completed - Japan ... 展开 >> 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 收起 <<
NCT03279289 Metastatic Colorectal Cancer Phase 2 Recruiting July 2021 Spain ... 展开 >> 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 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.48mL

0.90mL

0.45mL

22.39mL

4.48mL

2.24mL

44.79mL

8.96mL

4.48mL

参考文献

[1]Minnaard-Huiban M, Emmen JM, et al. Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats: discordant enantioselectivity versus reduction of plasma aldosterone. Endocrinology. 2008 Jan;149(1):28-31.

[2]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;34(2):725-736.