PT2977 (Synonyms: PT2977; MK-6482) |
| Catalog No.GC37034 |
PT2977(PT2977)은 경구 활성 및 선택적 HIF-2α입니다. IC50이 9nM인 억제제. PT2977, 2세대 HIF-2α 억제제, 효능을 증가시키고 약동학 프로파일을 개선합니다. PT2977은 투명 세포 신세포 암종(ccRCC)에 대한 잠재적 치료제입니다.
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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