2. Protein Tyrosine Kinase/RTK Autophagy
  3. Bcr-Abl FGFR PDGFR VEGFR Src Autophagy
  4. Ponatinib hydrochloride

Ponatinib hydrochloride  (Synonyms: AP24534 hydrochloride)

Art. -Nr.: HY-108766 Reinheit: 99.76%
COA
SDS
Handling Instructions Technical Support

Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.

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CAS. Nr. : 1114544-31-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
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Based on 50 publication(s) in Google Scholar

Other Forms of Ponatinib hydrochloride:

Ponatinib hydrochloride Related Antibodies

Top Publications Citing Use of Products

50 Publications Citing Use of MCE Ponatinib hydrochloride

WB
Cell Imaging/Staining
In Vivo Efficacy Study
Cell Proliferation/Viability Assay

    Ponatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Dec 2:138305.  [Abstract]

    KBM5-T315I cells were treated with the indicated concentrations of CX-4945, Ponatinib (0.001-10 μM), or with two combined drugs by simultaneously increasing their concentration at the ratio of 1:500 for Ponatinib + CX-4945. Viability was assessed by the MTT method after 48 h treatment and expressed as percentage of vehicle-treated controls.

    Ponatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117569.  [Abstract]

    Ponatinib inhibited proliferation of CCA cell lines. Relative viability (%) of KKU-100 and KKU-213A cells after 48 h treatment with buparlisib, Ponatinib and the combination of both drugs (0.25-5 μM).

    Ponatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117569.  [Abstract]

    Intracellular ROS in KKU-100 and KKU-213A cells after exposure to 0.75 μM Buparlisib, 0.75 μM Ponatinib and the combination of both for 6 h was measured by fluorescence microscopy using DCFH-DA staining.

    Ponatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2024 Nov:180:117569.  [Abstract]

    Representative image of tumors dissected from KKU-213A xenograft mice after 14 days of treatment with Buparlisib (15 mg/kg/day), Ponatinib (30 mg/kg/day) and their combination.

    Ponatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Oct;13(10):4253-4272.  [Abstract]

    BxPC-3, PANC-1 and H6c7 cells were treated with ponatinib (0.1–20 μM) for 24 h, and then cell viability was analyzed by CCK-8 assay.

    Ponatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharm Sin B. 2023 Oct;13(10):4253-4272.  [Abstract]

    PANC-1 cells were treated with Ponatinib (5-20 μM) or Perifosine (30-70 μM) for 24 h, and total cellular extracts were subjected to Western blot analyses using antibodies against GSDMD and β-tubulin.

    Ponatinib hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Hematol. 2014 May;42(5):369-379.e3.  [Abstract]

    Phosphorylation levels of F/P (or its mutant), STAT5, or ERK in lysates of CMPs expressing Hes1 with F/P, F/P-D842V, or F/P-T674I, which have been treated with indicated doses of Ponatinib (0.1-1 μM) for 15 min. Data are representative of three independent experiments.

    Alle Bcr-Abl Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    Abl Bcr-Abl

    Alle PDGFR Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    PDGFR PDGFRβ PDGFRα

    Alle VEGFR Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    Alle Src Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

    • Biologische Aktivität

    • Reinheit & Dokumentation

    • Verweise

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    Beschreibung

    Ponatinib hydrochloride (AP24534 hydrochloride) is a hydrochloride of ponatinib. Ponatinib is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively[1].

    IC50 & Target

    LYN

    0.24 nM (IC50)

    Abl

    0.37 nM (IC50)

    PDGFRα

    1.1 nM (IC50)

    VEGFR2

    1.5 nM (IC50)

    FGFR1

    2.2 nM (IC50)

    Src

    5.4 nM (IC50)

    In Vitro

    Ponatinib hydrochloride (0.11, 017 μM, 24-48 h) can reduce the viability, migration, and function of human endothelial cells[2].

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

    Ponatinib hydrochloride Related Antibodies

    Cell Viability Assay[2]

    Cell Line: HUVEC
    Concentration: 0-20 μM
    Incubation Time: 48 h
    Result: Decreased cell viability in a dose-dependent manner with IC50 value of 0.55 μM.

    Apoptosis Analysis[2]

    Cell Line: HUVEC
    Concentration: 0.11, 0.17 μM
    Incubation Time: 24 h
    Result: Increased the percentage of annexin/PI labeled cells.

    Cell Migration Assay [2]

    Cell Line: HUVEC
    Concentration: 0.17 μM
    Incubation Time: 20 h
    Result: Reduced VEGF-induced migration from 100% to 62.3 ± 4.8%.
    In Vivo

    Ponatinib hydrochloride (dissolved in 25 mM citrate buffer (pH 2.75), 200 μL in volume, oral) protects mice from lethal influenza infection by inhibiting cytokine storm[3].

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

    Animal Model: Influenza A Virus Infected Mice[3]
    Dosage: 200 μL, dissolved in 25 mM citrate buffer (pH 2.75)
    Administration: p.o.
    Result: Had higher survival rates and reduced the infiltration of neutrophils.
    Klinische Studie
    Molekulargewicht

    569.02

    Formel

    C29H28ClF3N6O
    CAS. Nr.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(C1=CC=C(C)C(C#CC2=CN=C3C=CC=NN23)=C1)NC4=CC=C(CN5CCN(CC5)C)C(C(F)(F)F)=C4.Cl
    Versand

    Room temperature in continental US; may vary elsewhere.
    Speicherung

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : 25 mg/mL (43.94 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7574 mL 8.7870 mL 17.5741 mL
    5 mM 0.3515 mL 1.7574 mL 3.5148 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molaritätsrechner

    • Verdünnungsrechner

    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 (4.39 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 (4.39 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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.
    Reinheit & Dokumentation

    Purity: 99.76%

    SDS (644 KB)

    COA (256 KB) HNMR (285 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    Verweise

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7574 mL 8.7870 mL 17.5741 mL 43.9352 mL
    5 mM 0.3515 mL 1.7574 mL 3.5148 mL 8.7870 mL
    10 mM 0.1757 mL 0.8787 mL 1.7574 mL 4.3935 mL
    15 mM 0.1172 mL 0.5858 mL 1.1716 mL 2.9290 mL
    20 mM 0.0879 mL 0.4394 mL 0.8787 mL 2.1968 mL
    25 mM 0.0703 mL 0.3515 mL 0.7030 mL 1.7574 mL
    30 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.4645 mL
    40 mM 0.0439 mL 0.2197 mL 0.4394 mL 1.0984 mL
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    Ponatinib hydrochloride 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:

    Ponatinib1114544-31-8AP24534AP 24534AP-24534Bcr-AblFGFRPDGFRVEGFRSrcAutophagyFibroblast growth factor receptorPlatelet-derived growth factor receptorVascular endothelial growth factor receptororally activemulti-targetedkinaseAblPDGFRαVEGFR2FGFR1Inhibitorinhibitorinhibit

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