Home ER stress & UPR HIF inhibitor Belzutifan (PT2977) For research use only.

Belzutifan (PT2977)

Synonyms: MK-6482

Belzutifan (PT2977), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC).

Belzutifan (PT2977) Chemical Structure

Belzutifan (PT2977) Chemical Structure

CAS: 1672668-24-4

Purity & Quality Control

Batch: S888601 DMSO] 77 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.79%
99.79

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Biological Activity

Description Belzutifan (PT2977), an orally active and selective HIF-2α inhibitor, increases potency and improves pharmacokinetic profile, providing a potential treatment for clear cell renal cell carcinoma (ccRCC).
Targets
HIF-2α [1]
9 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04994522 Recruiting End Stage Renal Disease|Renal Impairment Merck Sharp & Dohme LLC July 12 2022 Phase 1
NCT04846920 Active not recruiting Carcinoma Renal Cell Merck Sharp & Dohme LLC June 14 2021 Phase 1
NCT04627064 Recruiting Clear Cell Renal Cell Carcinoma Dana-Farber Cancer Institute|Eli Lilly and Company December 31 2020 Phase 1
NCT04489771 Active not recruiting Carcinoma Renal Cell Merck Sharp & Dohme LLC September 13 2020 Phase 2
NCT03634540 Active not recruiting Renal Cell Carcinoma (RCC)|Clear Cell Renal Cell Carcinoma (ccRCC)|Kidney Cancer|Renal Cancer|Renal Cell Carcinoma|Renal Cell Cancer Metastatic|Renal Cell Carcinoma Recurrent|Renal Cell Cancer Recurrent|Kidney Peloton Therapeutics Inc. a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA) September 27 2018 Phase 2
NCT03401788 Active not recruiting VHL - Von Hippel-Lindau Syndrome|VHL Gene Mutation|VHL Syndrome|VHL Gene Inactivation|VHL-Associated Renal Cell Carcinoma|VHL-Associated Clear Cell Renal Cell Carcinoma Peloton Therapeutics Inc. a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA) May 2 2018 Phase 2

Chemical lnformation & Solubility

Molecular Weight 383.34 Formula

C17H12F3NO4S
CAS No. 1672668-24-4 SDF --
Smiles CS(=O)(=O)C1=C2C(C(C(C2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)F)F)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 77 mg/mL ( (200.86 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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