Belzutifan
Belzutifan is a first-in-class oral HIF-2alpha inhibitor that blocks the dimerisation of HIF-2alpha (EPAS1) with ARNT, preventing transcription of hypoxia-response genes including VEGF, EPO, and GLUT1. In VHL-deficient tumours, constitutive HIF-2alpha activity drives tumorigenesis. FDA-approved for VHL disease-associated RCC, CNS haemangioblastomas, and pancreatic NETs.
Description
Scientific Overview: Belzutifan is a first-in-class oral HIF-2alpha inhibitor that blocks the dimerisation of HIF-2alpha (EPAS1) with ARNT, preventing transcription of hypoxia-response genes including VEGF, EPO, and GLUT1. In VHL-deficient tumours, constitutive HIF-2alpha activity drives tumorigenesis. FDA-approved for VHL disease-associated RCC, CNS haemangioblastomas, and pancreatic NETs.
Mechanism of Action: HIF-2alpha (EPAS1) Inhibitor
Purity: ≥99% | Molecular Formula: C20H14F3N3O2S
For Research Use Only. Not intended for diagnostic, therapeutic, or clinical applications.
Additional information
| Effect | HIF-2alpha (EPAS1) Inhibitor |
|---|---|
| Purity | ≥99% |
| Molecular Formula | C20H14F3N3O2S |
| CAS Number | 1672668-24-4 |
