Belzutifan | HIF-2α inhibitor

Belzutifan chemical structure

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Belzutifan (1672668-24-4) is a potent hypoxia-inducible factor 2α (HIF-2α) inhibitor (IC50 = 9 nM).1  Active in vivo in mouse and human studies of renal cell and non-renal cell carcinoma associated with VHL disease.1,2 An important toll for modulating the hypoxic tumor microenvironment.3 FDA approved for the treatment of von Hippel-Lindau associated diseases.

References/Citations:

  1. Xu et al. (2019), 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. 62 6876
  2. Fallah et al. (2022), FDA Approval Summary: Belzutifan for von Hippel-Lindau Disease-Associated Tumors; Clin. Cancer Res. 28 4843
  3. Cowman and koh (2021), Revisiting the HIF Switch in the Tumor and its Immune Microenvironment; Trends Cancer 8 28
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Alternate Name:
PT2977; MK-6482

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Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

Belzutifan (1672668-24-4) is a potent hypoxia-inducible factor 2α (HIF-2α) inhibitor (IC50 = 9 nM).1  Active in vivo in mouse and human studies of renal cell and non-renal cell carcinoma associated with VHL disease.1,2 An important toll for modulating the hypoxic tumor microenvironment.3 FDA approved for the treatment of von Hippel-Lindau associated diseases.

References/Citations:

  1. Xu et al. (2019), 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. 62 6876
  2. Fallah et al. (2022), FDA Approval Summary: Belzutifan for von Hippel-Lindau Disease-Associated Tumors; Clin. Cancer Res. 28 4843
  3. Cowman and koh (2021), Revisiting the HIF Switch in the Tumor and its Immune Microenvironment; Trends Cancer 8 28