Belzutifan | HIF-2α inhibitor

CAS:
 1672668-24-4
Catalog Number:
 10-4274
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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CAS:
1672668-24-4
Catalog Number:
10-4274
Activity:
HIF-2α inhibitor
Chemical Names:
3-[[(1S,2S,3R)-2,3-Difluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl]oxy]-5-fluorobenzonitrile
Alternate Name:
PT2977; MK-6482
Molecular Weight:
383.34
Molecular Formula:

C17H12F3NO4S

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 1 year when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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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