Art. -Nr.: HY-125840

Belzutifan

(Synonyms: PT2977; MK-6482)

15 Cited Publications

Kundenbewertung

Based on 15 publication(s) in Google Scholar

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).

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Reinheit: 99.62%
CAS. Nr.: 1672668-24-4
Formel: C₁₇H₁₂F₃NO₄S
Molecular Weight:383.34

Speicherung:

-20°C, stored under nitrogen

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

Belzutifan Chemical Structure

CAS. Nr.: 1672668-24-4

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Publications (15)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: 9 nM (HIF-2α)^[1]

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1672668-24-4
Appearance Solid
Molecular Weight 383.34
Formel C₁₇H₁₂F₃NO₄S
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
Synonyms

PT2977; MK-6482
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

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

Publications (15)

All OthersBio/Physico-chemical AssayRT-PCRWB

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Journal Impact Factor

Cancer Discov

LKB1/ STK11 Is a Tumor Suppressor in the Progression of Myeloproliferative Neoplasms. [Abstract]

2021 Jun;11(6):1398-1410. PMID: 33579786

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.
Ann Rheum Dis

Epithelial HIF2α expression induces intestinal barrier dysfunction and exacerbation of arthritis. [Abstract]

2022 Jul 12;81(8):1119-1130. PMID: 35710307
Cancer Res

Hypoxic Memory Mediates Prolonged Tumor Intrinsic Type I Interferon Suppression to Promote Breast Cancer Progression. [Abstract]

2024 Oct 1;84(19):3141-3157. PMID: 38990731
Sci Adv

Hypoxia-responsive interaction between P-TEFb, BHLHE40, and Tim8-Tim13 regulates hypoxic gene transcription. [Abstract]

2026 May 22;12(21):eadz9295. PMID: 42160428
Acta Pharmacol Sin

Discovery and characterization of a novel HIF-2α agonist for the treatment of CKD-related renal anemia. [Abstract]

2025 Oct 1. PMID: 41034402
Int J Mol Sci

Uric Acid Induces Hepatocytes Ferroptosis Through HIF-2α/DMT1-Mediated Iron Overload. [Abstract]

2026 Mar 20;27(6):2833. PMID: 41898692
Biochim Biophys Acta Mol Basis Dis

Hypoxia-driven heterogeneous expression of α5 integrin in glioblastoma stem cells is linked to HIF-2α. [Abstract]

2024 Aug 16:167471. PMID: 39154793

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.
Transl Oncol

Targeting EPAS-1/HIF-2α Pathway to Address Endocrine Resistance in Luminal A Type Breast Cancer. [Abstract]

2025 May 19:57:102415. PMID: 40393248
FASEB J

Belzutifan Attenuates Choroidal Neovascularization by Suppressing the HIF-2α/PAI-1 Axis. [Abstract]

2026 Apr 15;40(7):e71740. PMID: 41954091
J Proteome Res

Metabolomic Profiling Reveals Key Metabolic Alterations in MCF7 Tamoxifen-Resistant Cells Following EPAS1 Inhibition. [Abstract]

2025 Aug 1;24(8):4070-4081. PMID: 40675783
Exp Cell Res

Human trophoblast stem cell-differentiated syncytiotrophoblasts as a model for hypoxia-enhanced secretion of the anti-angiogenic factor sFLT1. [Abstract]

2025 Oct 1;452(2):114773. PMID: 41005427
Anal Methods

Near-infrared carbon dots enable ultra-sensitive fluorometric detection of belzutifan: a novel approach for real-time therapeutic drug monitoring in cancer treatment. [Abstract]

2025 Dec 11;17(48):9887-9897. PMID: 41347412
Mol Pharmacol

Structural basis for the allosteric inhibition of hypoxia-inducible factor (HIF)-2 by belzutifan. [Abstract]

2022 Sep 27;102(6):MOLPHARM-AR-2022-000525. PMID: 36167425
bioRxiv

2026 Jan 2.
Elife

Mechanisms governing target search and binding dynamics of hypoxia-inducible factors. [Abstract]

2022 Nov 2:11:e75064. PMID: 36322456

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).

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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

Keywords

Belzutifan

15 Cited Publications

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Belzutifan

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Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Belzutifan

Alle HIF/HIF Prolyl-Hydroxylase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (15)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Belzutifan Related Classifications

HY-125840 Related Classifications