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 No. 1672668-24-4

Purity & Quality Control

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

Belzutifan (PT2977) Related Products

Signaling Pathway

HIF Signaling Pathways

HIF Signaling Pathway

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 Completed
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 Active not 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 Information & 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
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

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.

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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