Belzutifan (Synonyms: PT2977; MK-6482)

Name: Belzutifan
Brand: MedChemExpress
SKU: HY-125840
Rating: 5.0 (13 reviews)

Cat. No.: HY-125840 Purity: 99.62%: Data Sheet
COA

SDS
Handling Instructions
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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).

For research use only. We do not sell to patients.

CAS No. : 1672668-24-4

Size	Stock	Quantity

Free Sample (0.1 - 0.2 mg)	Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Belzutifan:

Belzutifan (Standard) In-stock

13 Publications Citing Use of MCE Belzutifan

Others

Bio/Physico-chemical Assay

RT-PCR

: Belzutifan purchased from MedChemExpress. Usage Cited in: Elife. 2022 Nov 2:11:e75064. [Abstract]; Luciferase assay using a hypoxia response element (HRE)-containing reporter confirms Belzutifan (0.2 nM-0.2 μM; 24 h) dosage-dependent inhibition of HIF-2α activity in wild-type (WT) 786-O cells.

: Belzutifan purchased from MedChemExpress. Usage Cited in: Elife. 2022 Nov 2:11:e75064. [Abstract]; Proportion of molecules as a function of diffusion coefficient for HIF-2α measured in Halo-HIF-2α knock-in (KIN) line clone A31 treated with different concentrations of Belzutifan (0.2 nM-0.2 μM; 24 h).

: Belzutifan purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2024 Aug 16:167471. [Abstract]; Analysis of the effect of treatments with specific HIF-2α antagonists on ITGA5 expression. Cells were treated with 20 μM Belzutifan or 20 μM Compound 2 for 24 h.

: Belzutifan purchased from MedChemExpress. Usage Cited in: Biochim Biophys Acta Mol Basis Dis. 2024 Aug 16:167471. [Abstract]; Analysis of the effect of treatments with specific HIF-2α antagonists on ITGA5 expression. Cells were treated with 20 μM Belzutifan or 20 μM Compound 2 for 72 h.

: Belzutifan purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2021 Jun;11(6):1398-1410. [Abstract]; Number of hematopoietic colonies generated by CD34+ progenitors from healthy donors treated with echinomycin, mitotempo, PP242, PT2977 (30-300 nM; 14 days) and ruxolitinib at various concentrations versus DMSO control.

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HIF-1α HIF

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

IC50: 9 nM (HIF-2α)^[1]

In Vitro

Belzutifan (PT2977) potently and dose-dependently reduces mRNA levels of human cyclin D1, a target gene regulated by HIF-2α, and leads to rapid and dose-dependent reduction in EPO expression^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

383.34

Formula

C₁₇H₁₂F₃NO₄S

CAS No.

1672668-24-4

Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (130.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Acetone : 50 mg/mL (130.43 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6087 mL	13.0433 mL	26.0865 mL
5 mM	0.5217 mL	2.6087 mL	5.2173 mL
10 mM	0.2609 mL	1.3043 mL	2.6087 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: ≥ 0.5 mg/mL (1.30 mM); Clear solution

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 1 year; -20°C, 6 months (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.73% ee.: 98.40%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (254 KB) HNMR (198 KB) NP-HPLC (128 KB) LCMS (119 KB)

Handling Instructions (2659 KB)

References

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / Acetone	1 mM	2.6087 mL	13.0433 mL	26.0865 mL	65.2163 mL
	5 mM	0.5217 mL	2.6087 mL	5.2173 mL	13.0433 mL
	10 mM	0.2609 mL	1.3043 mL	2.6087 mL	6.5216 mL
	15 mM	0.1739 mL	0.8696 mL	1.7391 mL	4.3478 mL
	20 mM	0.1304 mL	0.6522 mL	1.3043 mL	3.2608 mL
	25 mM	0.1043 mL	0.5217 mL	1.0435 mL	2.6087 mL
	30 mM	0.0870 mL	0.4348 mL	0.8696 mL	2.1739 mL
	40 mM	0.0652 mL	0.3261 mL	0.6522 mL	1.6304 mL
	50 mM	0.0522 mL	0.2609 mL	0.5217 mL	1.3043 mL
	60 mM	0.0435 mL	0.2174 mL	0.4348 mL	1.0869 mL
	80 mM	0.0326 mL	0.1630 mL	0.3261 mL	0.8152 mL
	100 mM	0.0261 mL	0.1304 mL	0.2609 mL	0.6522 mL

Belzutifan Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Belzutifan1672668-24-4PT2977 MK-6482PT 2977PT-2977MK6482MK 6482MK-6482HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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Belzutifan (Synonyms: PT2977; MK-6482)

Customer Review

Other Forms of Belzutifan:

Belzutifan Related Antibodies

13 Publications Citing Use of MCE Belzutifan

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All HIF/HIF Prolyl-Hydroxylase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Belzutifan Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Belzutifan Related Classifications

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Customer Review

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