2. Metabolic Enzyme/Protease
  3. HIF/HIF Prolyl-Hydroxylase
  4. Belzutifan

Belzutifan  (Synonyms: PT2977; MK-6482)

Cat. No.: HY-125840 Purity: 99.85%
COA 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.

Belzutifan Chemical Structure

Belzutifan Chemical Structure

CAS No. : 1672668-24-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 209 In-stock
Solution
10 mM * 1 mL in DMSO USD 209 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 190 In-stock
10 mg USD 280 In-stock
25 mg USD 525 In-stock
50 mg USD 840 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 6 publication(s) in Google Scholar

Belzutifan Related Antibodies

Top Publications Citing Use of Products

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

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HIF-1α HIF

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1].

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.

Belzutifan Related Antibodies
Clinical Trial
Molecular Weight

383.34

Formula

C17H12F3NO4S
CAS No.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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: 99.85%

COA (254 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

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.

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
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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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