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

PT-2385 

Cat. No.: HY-12867 Purity: 99.48%
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
10 mM * 1 mL in DMSO USD 160 In-stock
Estimated Time of Arrival: December 31
2 mg USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 190 In-stock
Estimated Time of Arrival: December 31
10 mg USD 330 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1300 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 15 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

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

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

    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.

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

    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 MCE. Usage Cited in: Nat Commun. 2020 Oct 6;11(1):5005.

    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.
    • Biological Activity

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    • 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].

    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].

    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.

    1672665-49-4

    SMILES

    N#CC1=CC(F)=CC(OC2=CC=C(S(=O)(C)=O)C3=C2CC(F)(F)[[email protected]]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 6 months
      -20°C 1 month
    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:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    • 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

    • 3.

      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 provided by MCE.
    References

    Purity: 99.48%

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    Keywords:

    PT-2385PT2385PT 2385HIF/HIF Prolyl-HydroxylaseHypoxia-inducible factorsHIFsHIF-PHInhibitorinhibitorinhibit

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    Product Name:
    PT-2385
    Cat. No.:
    HY-12867
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