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

Belzutifan  (Synonyms: PT2977; MK-6482)

製品番号: HY-125840 純度: 99.62%
COA 取扱説明書 Technical Support

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).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 1672668-24-4

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 209 在庫あり
Solution
10 mM * 1 mL in DMSO USD 209 在庫あり
Solid
5 mg $190 在庫あり
10 mg $280 在庫あり
25 mg $525 在庫あり
50 mg $840 在庫あり
100 mg $1350 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

カスタマーレビュー

Based on 13 publication(s) in Google Scholar

Other Forms of Belzutifan:

Belzutifan 関連抗体

Top Publications Citing Use of Products

    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.

    HIF/HIF Prolyl-Hydroxylase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    HIF-1α HIF

    • 生物活性

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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]
    体外実験

    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 関連抗体
    臨床実験
    分子量

    383.34

    分子式

    C17H12F3NO4S
    CAS 番号
    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    -20°C, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
    溶剤 & 溶解度
    体外: 

    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)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

    C1

    ×
    体積 （開始）

    V1

    =
    濃度 （終了）

    C2

    ×
    体積 （終了）

    V2

    体内:

    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.
    純度とドキュメンテーション

    純度: 99.73% ee.: 98.40%

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

    取扱説明書 (2659 KB)
    参考文献

    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

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    質量   濃度   体積   分子量 *
    = × ×

    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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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    製品名:
    Belzutifan
    製品番号:
    HY-125840
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