PT2977

Modify Date: 2024-01-08 18:13:08

PT2977 Structure
PT2977 structure
Common Name PT2977
CAS Number 1672668-24-4 Molecular Weight 383.34
Density N/A Boiling Point N/A
Molecular Formula C17H12F3NO4S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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) and von Hippel–Lindau (VHL) disease[1].

 Names

Name PT2977

 PT2977 Biological Activity

Description 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].
Related Catalog
Target

HIF-2α:9 nM (IC50)

In Vitro 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C17H12F3NO4S
Molecular Weight 383.34