Belzutifan 是具有口服活性的HIF-2α选择性抑制剂，IC50为 9 nM。Belzutifan具有提高的效力和改善的药代动力学特征。Belzutifan可以抑制透明细胞肾细胞癌。

PT2977 is a potential treatment for clear cell renal cell carcinoma (ccRCC). PT2977 is an orally active and selective HIF-2α inhibitor (IC50: 9 nM). PT2977, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile.

PT2977 effectively and dose-dependently decreased mRNA levels of human cyclin D1, a target gene regulated by HIF-2α. It leads to a rapid and dose-dependent reduction in EPO expression[1].

1672668-24-4

C17H12F3NO4S

383.34

PT2977;MK-6482

DMSO:50 mg/mL (130.43 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years