產品屬性：
產品名稱 | PT2977 |
規格 | 10 mM * 1 mL in DMSO、1mg、5mg、10mg |
貨號 | EY-01Y12607 |
Cas No.: 1672668-24-4
別名: N/A
化學名: N/A
分子式: C17H12F3NO4S
分子量: 383.34
溶解度: DMSO: 50 mg/mL (130.43 mM)
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
PT2977 is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. PT2977 is a potential treatment for Clear cell renal cell carcinoma (ccRCC) and von Hippel-Lindau (VHL) disease[1].IC50: 9 nM (HIF-2α)[1]PT2977 potently and dose-dependently reduces mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, and leads to rapid and dose-dependent reduction in EPO expression[1].[1]. Xu R, et al. 3-[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonylindan-4-yl]oxy-5-fluorobenzonitrile (PT2977), a Hypoxia-Inducible Factor 2α (HIF-2α) Inhibitor for the Treatment of Clear Cell Renal Cell Carcinoma. J Med Chem. 2019 Aug 8;62(15):6876-6893.
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