PT2977

Catalog No.S8886 Synonyms: Belzutifan, MK-6482

For research use only.

PT2977 (Belzutifan, MK-6482), 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).

PT2977 Chemical Structure

CAS No. 1672668-24-4

Purity & Quality Control

Choose Selective HIF Inhibitors

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Biological Activity

Description PT2977 (Belzutifan, MK-6482), 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

Protocol (from reference)

Chemical Information

Molecular Weight 383.34
Formula

C17H12F3NO4S

CAS No. 1672668-24-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CS(=O)(=O)C1=C2C(C(C(C2=C(C=C1)OC3=CC(=CC(=C3)C#N)F)F)F)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04994522 Recruiting Drug: Belzutifan End Stage Renal Disease|Renal Impairment Merck Sharp & Dohme LLC July 12 2022 Phase 1
NCT04846920 Recruiting Drug: Belzutifan Carcinoma Renal Cell Merck Sharp & Dohme LLC June 14 2021 Phase 1
NCT04627064 Recruiting Drug: Abemaciclib|Drug: MK-6482 Clear Cell Renal Cell Carcinoma Dana-Farber Cancer Institute|Eli Lilly and Company December 31 2020 Phase 1
NCT04489771 Active not recruiting Drug: Belzutifan Carcinoma Renal Cell Merck Sharp & Dohme LLC September 13 2020 Phase 2
NCT03634540 Recruiting Drug: Belzutifan|Drug: Cabozantinib 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. September 27 2018 Phase 2
NCT03401788 Active not recruiting Drug: Belzutifan 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. May 2 2018 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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