Belzutifan

• CAT Number: I018717
• CAS Number: 1672668-24-4
• Molecular Formula: C₁₇H₁₂F₃NO₄S
• Molecular Weight: 383.34
• Purity: 98%
• Target: HIF/HIF Prolyl-Hydroxylase
• Target Protein: Q99814
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: IC50: 9 nM (HIF-2α)
• IUPAC Name: 3-[[(1S,2S,3R)-2,3-difluoro-1-hydroxy-7-methylsulfonyl-2,3-dihydro-1H-inden-4-yl]oxy]-5-fluorobenzonitrile
• InChI: 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
• InChIKey: LOMMPXLFBTZENJ-ZACQAIPSSA-N
• SMILES: CS(=O)(=O)C1=C2[C@@H]([C@@H]([C@@H](C2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)F)F)O

Belzutifan（Cat No.:I018717）is a novel hypoxia-inducible factor-2 alpha (HIF-2α) inhibitor used to treat patients with von Hippel-Lindau (VHL) disease-associated renal cell carcinoma (RCC) and other tumors. By inhibiting HIF-2α, a key driver of tumor growth in VHL, belzutifan reduces the expression of genes involved in angiogenesis and tumor survival. This targeted mechanism disrupts the adaptation of cancer cells to hypoxic conditions, slowing tumor progression. Belzutifan offers an effective, oral treatment option for VHL-related tumors, providing benefits in managing cancer with a favorable safety profile.

Reference

[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.