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Fadrozole hydrochloride

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Chemical Structure| 102676-31-3 同义名 : CGS 16949A;(Rac)-FAD286 hydrochloride;Fadrozole (hydrochloride)
CAS号 : 102676-31-3
货号 : A856566
分子式 : C14H14ClN3
纯度 : 98%+
分子量 : 259.734
MDL号 : MFCD00866239
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(404.26 mM)，配合低频超声，并水浴加热至45℃助溶，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

H2O: 100 mg/mL(385.01 mM)，配合低频超声助溶
动物实验配方：
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... 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

3.85mL

0.77mL

0.39mL

19.25mL

3.85mL

1.93mL

38.50mL

7.70mL

3.85mL
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.