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编 号:F196901
分子式:C26H23N5O2
分子量:437.49
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
Alobresib (GS-5829) is a BET bromodomain inhibitor, which represents a highly effective therapeutics agent against recurrent/chemotherapy resistant uterine serous carcinoma (USC) overexpressing c-Myc. Alobresib can be used in the metastatic castration-resistant prostate cancer (mCRPC) research.

体内研究:
Alobresib (10 和 20 mg/kg;口服;每天两次;持续 28 天) 在雌性 CB17/lcrHsd-Prkd/scid 小鼠中抑制 USC-ARK2 异种移植肿瘤的生长。与 每天接受 JQ1 (50 mg/kg/天 ip) 处理及媒介物对照小鼠相比,Alobresib 在小鼠体内表现出明显更慢的肿瘤生长速率。 Alobresib (10 和 20 mg/kg;口服;每天两次;持续 28 天) 具有良好的耐受性,与对照组相比,对体重没有明显影响。Animal Model:Female CB17/lcrHsd-Prkd/scid mice (15-19 g) bearing USC-ARK2 tumors
Dosage:10 and 20 mg/kg
Administration:Oral; twice-daily; 28 days
Result:Exhibited a significantly slower rate of tumor growth, compared with vehicle control and to mice undergoing daily treatment with JQ1 (50 mg/kg/day i.p.).

体外研究:
Alobresib (0.1 nM-100 μM;72 小时) 抑制原发性子宫浆液性癌 (USC) 细胞系中的细胞增殖。
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