1. Metabolic Enzyme/Protease
  2. HIF/HIF Prolyl-Hydroxylase
  3. PT-2385

PT-2385 est un inhibiteur sélectif du HIF-2α avec un Ki de moins de 50 nM.

PT-2385 ist ein selektiver HIF-2α-Inhibitor mit einem Ki von weniger als 50 nM.

PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM.

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

PT-2385 Chemical Structure

PT-2385 Chemical Structure

CAS No. : 1672665-49-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 160 In-stock
Solution
10 mM * 1 mL in DMSO USD 160 In-stock
Solid
2 mg USD 110 In-stock
5 mg USD 190 In-stock
10 mg USD 330 In-stock
50 mg   Get quote  
100 mg   Get quote  

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

Customer Review

Based on 36 publication(s) in Google Scholar

Top Publications Citing Use of Products

32 Publications Citing Use of MCE PT-2385

WB

    PT-2385 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Oct 6;11(1):5005.  [Abstract]

    WT naïve CD4+ T cells are activated by CD3/CD28 (2/1 μg/mL) in the presence of HIF-2α inhibitor PT2385 for 2 days, or activating WT iTreg cells are treated with 10 μM PT2385, and HIF-1α levels determined. Treatment of activating WT CD4+ T cells with PT2385 leads to dose-dependent upregulation of HIF-1α. PT2385 also increases the level of HIF-1α induction in activated WT iTreg cells.

    PT-2385 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2019 Jan 22;508(4):1233-1239.  [Abstract]

    Western blot with HIF2a-specific antibody on lysates from LAN-1 cells treated grown in normoxia (21% O2) or in hypoxia (1% O2), with the indicated concentration of PT2385.

    PT-2385 purchased from MedChemExpress. Usage Cited in: Nat Med. 2017 Nov;23(11):1298-1308.  [Abstract]

    Western blot analysis of NEU3 protein expression in the small intestine.

    PT-2385 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Oct 12;8(10):e3095.  [Abstract]

    Western blot assays show PT-2385 can suppress HIF-2α level and partly reverse the decrease of AR and the increase of downstream signals (pSTAT3, pAKT and pERK) by Bay 43-9006 treatment.

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

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PT-2385 is a selective HIF-2α inhibitor with a Ki of less than 50 nM[1][2].

    IC50 & Target

    Kd: <50 nM (HIF-2α)[1]

    In Vitro

    PT-2385 (PT2385) is a selective antagonist of HIF-2 over HIF-1. PT-2385 is inactive for HIF-1α[1].

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

    In Vivo

    PT-2385 (30 or 100 mg/kg; oral gavage; twice daily) result in a rapid, dose-dependent tumor regression[3].
    PT-2385 (PT2385) inhibits expression of HIF-2α regulated genes in a dose dependent manner in vivo. Tumor is regressed with PT-2385 (3 and 10 mg/kg, p.o., b.i.d. dose) in 786-O xenograft. PT-2385 (1,3 and 10 mg/kg) also inhibits tumor-derived VEGFA protein levels. PT-2385 (10 mg/kg) treatment reduces proliferation (Ki67) and angiogenesis (CD-31)[1].

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

    Animal Model: SCID/beige mice with the 786-O and A498 RCC cell lines[3]
    Dosage: 30 or 100 mg/kg
    Administration: Oral gavage; twice daily
    Result: Resulted in a rapid, dose-dependent tumor regression.
    Clinical Trial
    Molecular Weight

    383.34

    Formula

    C17H12F3NO4S

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2CC(F)(F)[C@H]3O)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

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

    *"≥" means soluble, but saturation unknown.

    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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. 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
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    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: 2.87 mg/mL (7.49 mM); Suspended solution; Need ultrasonic

    • Protocol 2

      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.
    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).
    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: 99.48%

    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 years; -20°C, 6 months. When stored at -80°C, please use it within 1 years. 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 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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    PT-2385 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.

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    Product Name:
    PT-2385
    Cat. No.:
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