PT2977 (Synonyms: PT2977; MK-6482) |
| رقم الكتالوجGC37034 |
PT2977 (PT2977) هو HIF-2α نشط شفهيًا وانتقائيًا ؛ مثبط مع IC 50 من 9 نانومتر. PT2977 ، باعتباره الجيل الثاني من HIF-2α ؛ مثبط ، يزيد من الفاعلية ويحسن الصورة الحركية الدوائية. PT2977 هو علاج محتمل لسرطان الخلايا الكلوية الصافية (ccRCC).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1672668-24-4
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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