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Belzutifan

Name: Belzutifan
Brand: TargetMol
SKU: T16679
Price: 64 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: PT2977, MK-6482) Copy Product Info

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Synonyms: PT2977, MK-6482

Catalog No. T16679 Copy Product Info

Purity: 99.88%

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Belzutifan (MK-6482, PT2977) is a small-molecule inhibitor and a HIF-2α inhibitor (IC50 = 9 nM) with high selectivity, oral activity, and improved pharmacokinetic characteristics, used for the treatment of clear cell renal cell carcinoma and related VHL diseases.

Cas No. 1672668-24-4

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Pack Size	Price	USA Stock	Global Stock
1 mg	$64	In Stock	In Stock
5 mg	$155	In Stock	In Stock
10 mg	$228	In Stock	In Stock
25 mg	$433	In Stock	In Stock
50 mg	$695	In Stock	In Stock
100 mg	$987	In Stock	In Stock
200 mg	$1,330	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$169	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.88%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Belzutifan (MK-6482, PT2977) is a small-molecule inhibitor and a HIF-2α inhibitor (IC50 = 9 nM) with high selectivity, oral activity, and improved pharmacokinetic characteristics, used for the treatment of clear cell renal cell carcinoma and related VHL diseases.
Targets & IC50	HIF2α:9 nM
In vitro	Methods: Cell proliferation assays and CRISPR functional experiments were used to detect the in vitro activity of Belzutifan. VHL-deficient clear cell renal cell carcinoma OSRC2, TUHR4TKB, and 786-O cells were selected and incubated with 2 μM drug for 16 days, with HIF2α knockout groups set as controls. Results: Belzutifan significantly inhibited cell proliferation, blocked HIF2α binding to ARNT, and downregulated CCND1 expression; sustained overexpression of Cyclin D1 in cells reversed the proliferation inhibitory effect of Belzutifan. [1] Methods: VHL-deficient clear cell renal cell carcinoma (ccRCC) cells were selected and incubated with gradient concentrations of Belzutifan to detect HIF-2α target gene expression and cell proliferation changes. Results: Belzutifan specifically blocked HIF-2α dimerization with ARNT, significantly downregulated pro-oncogenic gene expression, and effectively inhibited ccRCC cell proliferation in a dose-dependent manner, providing evidence for in vivo antitumor activity. [2]
In vivo	Methods: A clear cell renal cell carcinoma xenograft mouse model was used. Belzutifan was administered by oral gavage at doses set according to preclinical equivalent regimens, once daily for 21–28 consecutive days, with a vehicle of 0.5% methylcellulose, PEG400, and ethanol mixture, and a blank vehicle control group was established. Results: Belzutifan significantly inhibited tumor growth, downregulated HIF-2α target gene expression in tumor tissue, reduced VEGF and Cyclin D1 levels, showed no significant body weight loss or organ toxicity, and demonstrated definite in vivo antitumor activity with good tolerability. [3]
Synonyms	PT2977, MK-6482

Chemical Properties

Molecular Weight	383.34
Formula	C₁₇H₁₂F₃NO₄S
Cas No.	1672668-24-4
Smiles	CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@@H](F)[C@@H](F)[C@@H](O)c12
Relative Density.	1.56 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Store under nitrogen,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 50.5 mg/mL (131.74 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.22 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6087 mL	13.0433 mL	26.0865 mL	130.4325 mL
5 mM	0.5217 mL	2.6087 mL	5.2173 mL	26.0865 mL
10 mM	0.2609 mL	1.3043 mL	2.6087 mL	13.0433 mL
20 mM	0.1304 mL	0.6522 mL	1.3043 mL	6.5216 mL
50 mM	0.0522 mL	0.2609 mL	0.5217 mL	2.6087 mL
100 mM	0.0261 mL	0.1304 mL	0.2609 mL	1.3043 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.