A HIF-2α inhibitor
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Isomer(s)
21325PT2385
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Belzutifan

Item No. 39652

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[(1S,2S,3R)-2,3-difluoro-2,3-dihydro-1-hydroxy-7-(methylsulfonyl)-1H-inden-4-yl]oxy]-5-fluoro-benzonitrile
CAS Number
1672668-24-4
Synonyms
  • MK-6482
  • PT2977
Molecular Formula
C17H12F3NO4S
Formula Weight
383.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
CS(=O)(C1=C2C([C@H]([C@H]([C@H]2O)F)F)=C(C=C1)OC3=CC(F)=CC(C#N)=C3)=O
InChi Code
InChI=1S/C17H12F3NO4S/c1-26(23,24)12-3-2-11(13-14(12)17(22)16(20)15(13)19)25-10-5-8(7-21)4-9(18)6-10/h2-6,15-17,22H,1H3/t15-,16-,17+/m1/s1
InChi Key
LOMMPXLFBTZENJ-ZACQAIPSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

    $616

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    Cayman Chemical
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    Product Description

    Belzutifan is an inhibitor of hypoxia-inducible factor-2α (HIF-2α).1,2 It inhibits HIF-2α heterodimerization with the aryl hydrocarbon receptor nuclear translocator (ARNT) PAS-B domain in a cell-free assay (Ki = 23 nM), activation of HIF-2α in a reporter assay using 786-O renal cell carcinoma cells (IC50 = 17 nM), and secretion of the HIF-2α target VEGF-A from 786-O cells (EC50 = 17 nM). Belzutifan (0.3-3 mg/kg) induces tumor regression in a 786-O mouse xenograft model.2 It reduces hematocrit levels and right ventricular pressure in mice expressing an arginine-to-tryptophan mutation at position 200 in the von Hippel-Lindau protein (VHLR200W) in a model of Chuvash polycythemia when administered at a dose of 0.1 mg/g.3 Formulations containing belzutifan have been used in the treatment of VHL disease-associated cancers.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ren, X., Diao, X., Zhuang, J., et al. Structural basis for the allosteric inhibition of hypoxia-inducible factor 2 by belzutifan. Mol. Pharmacol. MOLPHARM-AR-2022-000525, (2022).

    2. Xu, R., Wang, K., Rizzi, J.P., et al. 3-[(1 S,2 S,3 R)-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(15), 6876-6893 (2019).

    3. Ghosh, M.C., Zhang, D.-L., Ollivierre, W.H., et al. Therapeutic inhibition of HIF-2α reverses polycythemia and pulmonary hypertension in murine models of human diseases. Blood 137(18), 2509-2519 (2021).