Belzutifan

Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) [1].

Product Specifications

CAS Number

[1672668-24-4]

Product Name Alternative

PT2977; MK-6482

UNSPSC

12352005

Hazard Statement

H315, H319, H320

Target

HIF/HIF Prolyl-Hydroxylase

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/pt2977.html

Concentration

10mM

Purity

99.85

Solubility

Acetone : 50 mg/mL (ultrasonic) |DMSO : 50 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2[C@@H](F)[C@@H](F)[C@H]3O)=C1

Molecular Formula

C17H12F3NO4S

Molecular Weight

383.34

Precautions

H315, H319, H320

References & Citations

[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.