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PT2977 (Synonyms: PT2977; MK-6482)

Catalog No.GC37034

PT2977 (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).

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PT2977 Chemical Structure

Cas No.: 1672668-24-4

Size Price Stock Qty
10mM (in 1mL DMSO)
$382.00
In stock
5mg
$133.00
In stock
10mg
$196.00
In stock
25mg
$368.00
In stock
50mg
$588.00
In stock

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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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Average Rating: 5 ★★★★★ (Based on Reviews and 17 reference(s) in Google Scholar.)

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