Name: Belzutifan (PT2977)
Brand: Selleck Chemicals
SKU: S8886
Rating: 5 (1 reviews)

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

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

Belzutifan (PT2977) Related Products

Related Targets	HIF1 HIF2 PHD1 PHD2 PHD3	Click to Expand
Related Compound Libraries	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ Highly Selective Inhibitor Library	Click to Expand

Signaling Pathway

HIF Signaling Pathway

Choose Selective HIF Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

[1] Xu R, et al. J Med Chem. 2019 Aug 8;62(15):6876-6893.

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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+ %

Calculation results:

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.

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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