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PT2977 (Synonyms: PT2977; MK-6482)

Katalog-Nr.GC37034

PT2977 (PT2977) ist ein oral aktiver und selektiver HIF-2α Inhibitor mit einem IC50 von 9 nM. PT2977 als HIF-2&7#945 der zweiten Generation; Inhibitor, erhÖht die Wirksamkeit und verbessert das pharmakokinetische Profil. PT2977 ist eine potenzielle Behandlung fÜr das klarzellige Nierenzellkarzinom (ccRCC).

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PT2977 Chemische Struktur

Cas No.: 1672668-24-4

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10mM (in 1mL DMSO)
382,00 $
Auf Lager
5mg
133,00 $
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10mg
196,00 $
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25mg
368,00 $
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50mg
588,00 $
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

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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