货号:A856566 同义名: CGS 16949A;(Rac)-FAD286 hydrochloride
Fadrozole HCl specifically inhibits aromatase, blocking the aromatization of androstenedione and testosterone into estrone and estradiol, respectively.
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Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
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产品名称 | Aromatase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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Obacunone |
+
Aromatase, IC50: 28.4 μM |
Nrf2 | 98% | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
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]. |
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 << |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 102676-31-3 |
分子式 | C14H14ClN3 |
分子量 | 259.734 |
别名 | CGS 16949A;(Rac)-FAD286 hydrochloride;Fadrozole (hydrochloride) |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
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 |