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

PT-2385 

Cat. No.: HY-12867 Purity: 98.97%
COA Handling Instructions

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)

    *"≥" 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
    10 mM 0.2609 mL 1.3043 mL 2.6087 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      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

    • 4.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.52 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.48%

    References
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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.:
    HY-12867
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