1. Protein Tyrosine Kinase/RTK
  2. FGFR
  3. Pemigatinib

Pemigatinib  (Synonyms: INCB054828)

製品番号: HY-109099 純度: 99.84%
COA 取扱説明書 Technical Support

Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma.

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CAS 番号 : 1513857-77-6

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カスタマーレビュー

Based on 21 publication(s) in Google Scholar

Other Forms of Pemigatinib:

Top Publications Citing Use of Products

    Pemigatinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 24.  [Abstract]

    Growth rate (GR)-corrected dose–response curves of NMuMG cells expressing indicated Fgfr2 variants and treated for 4 days with Pemigatinib (10-4-100 μM). Data are represented as mean ± SEM of n = 5 replicas per group.

    Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251.  [Abstract]

    T07 cells (5 × 105) were injected into the tail vein of approximately 6-week-old female BALB/c mice, and after 3 days mice were randomized prior to dosing of Pemigatinib at (25 mg/kg; oral gavage). BLI of vehicle vs pemigatinib-treated mice on days 10 and 14. The results showed that Pemigatinib significantly reduced pulmonary tumor burden in these mice.

    Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251.  [Abstract]

    4T07 cells were treated with Pemigatinib (Pemi, 10 nM) for the indicated amounts of time. Cells were lysed and analyzed by immunoblot for expression of PDGFR (α and β), ERK1/2 (phospho and total), and tubulin.

    Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251.  [Abstract]

    4T07 cells were treated with Pemigatinib (10 nM) for 24 h and cells were analyzed by RT-PCR for expression of PDGFRa and PDGFRb.

    Pemigatinib purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2025 Apr 4;16(1):251.  [Abstract]

    4T07 cells (2000 cells) were seeded under 3D culture conditions for 3 days at which point the cultures were left untreated (top row) or treated with Pemigatinib (50 nM; bottom row) for 96 h. Following drug treatment, cultures were allowed to recover in the absence or presence of PDGF-bb (100 ng/µL). Representative brightfield images are shown at the indicated days and treatment conditions.

    Pemigatinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Aug;608(7923):609-617.  [Abstract]

    Half-maximum inhibitory concentration (IC50) value quantifications of 2D-grown NMuMG cells expressing GFP or the indicated Fgfr2 variants and treated with AZD4547 or Pemigatinib for 4 days. Data are the mean of 5 independent experiments (GFP, Fgfr2FL, Fgfr2ΔE18) or 1 experiment (other Fgfr2 variants).

    Pemigatinib purchased from MedChemExpress. Usage Cited in: Nature. 2022 Aug;608(7923):609-617.  [Abstract]

    Dose-response curves of indicated human cancer cell lines treated with Pemigatinib (0.01-105 nM) for 4 days.
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    製品説明

    Pemigatinib (INCB054828) is an orally active, selective FGFR inhibitor with IC50s of 0.4 nM, 0.5 nM, 1.2 nM, 30 nM for FGFR1, FGFR2, FGFR3, FGFR4, respectively. Pemigatinib has the potential for cholangiocarcinoma[1][2].

    IC50 & Target[2]

    FGFR1

    0.4 nM (IC50)

    FGFR2

    0.5 nM (IC50)

    FGFR3

    1.2 nM (IC50)

    FGFR4

    30 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A204 IC50
    18.4 nM
    Compound: 1
    Antiproliferation activity against human A204 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
    Antiproliferation activity against human A204 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
    [PMID: 38718625]
    AN3-CA GI50
    0.132 μM
    Compound: 3
    Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against human AN3-CA cells harboring FGFR2 K310R/N549K mutant assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    BaF3 GI50
    0.005 μM
    Compound: 3
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3 assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    BaF3 GI50
    2.073 μM
    Compound: 3
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR3-V555M mutant assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    BaF3 GI50
    4.495 μM
    Compound: 3
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 N535K mutant assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    BaF3 GI50
    > 5 μM
    Compound: 3
    Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    BaF3 GI50
    > 5 μM
    Compound: 3
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against mouse BaF3 cells harboring TEL-FGFR4 V550E mutant assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    J82 GI50
    4.286 μM
    Compound: 3
    Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against human J82 cells harboring FGFR3 K652E mutant assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    KMS-11 GI50
    0.232 μM
    Compound: 3
    Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
    Antiproliferative activity against human KMS-11 cells harboring FGFR3 Y373C mutant assessed as cell growth inhibition by CellTiter-Glo assay
    [PMID: 35436119]
    MDA-MB-453 IC50
    73.7 nM
    Compound: 1
    Antiproliferation activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant incubated for 72 hrs by CCK8 assay
    Antiproliferation activity against human MDA-MB-453 cells harboring FGFR4 Y367C mutant incubated for 72 hrs by CCK8 assay
    [PMID: 38718625]
    RT-112 IC50
    174 nM
    Compound: Pemigatinib
    Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    Antiproliferative activity against human RT-112 cells expressing FGFR3 K650M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    [PMID: 38267212]
    RT-112 IC50
    1880 nM
    Compound: Pemigatinib
    Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    Antiproliferative activity against human RT-112 cells expressing FGFR3 N540K mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    [PMID: 38267212]
    RT-112 IC50
    23.7 nM
    Compound: 1
    Antiproliferation activity against human RT-112 cells harboring FGFR3-TACC3 incubated for 72 hrs by CCK8 assay
    Antiproliferation activity against human RT-112 cells harboring FGFR3-TACC3 incubated for 72 hrs by CCK8 assay
    [PMID: 38718625]
    RT-112 IC50
    3.3 nM
    Compound: Pemigatinib
    Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    Antiproliferative activity against human RT-112 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    [PMID: 38267212]
    RT-112 IC50
    6 nM
    Compound: Pemigatinib
    Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    Antiproliferative activity against human RT-112 cells expressing FGFR3 assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    [PMID: 38267212]
    RT-112 IC50
    > 1150 nM
    Compound: Pemigatinib
    Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    Antiproliferative activity against human RT-112 cells expressing FGFR3 V555M mutant assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    [PMID: 38267212]
    SNU-16 IC50
    3.9 nM
    Compound: Pemigatinib
    Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 5 days by Cell-titer glo assay
    [PMID: 38267212]
    SNU-16 IC50
    5.9 nM
    Compound: 1
    Antiproliferation activity against human SNU-16 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
    Antiproliferation activity against human SNU-16 cells harboring FGFR2 amplification incubated for 72 hrs by CCK8 assay
    [PMID: 38718625]
    Sf9 IC50
    0.4 nM
    Compound: 2
    Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
    Inhibition of N-terminal GST tagged recombinant human FGFR2 (400 to 821 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
    [PMID: 36356320]
    Sf9 IC50
    1.7 nM
    Compound: 2
    Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
    Inhibition of N-terminal His-Avi tagged recombinant human FGFR3 (447 to 761 residues) expressed in an Sf9 infected baculovirus expression system using biotin-EQEDEPEGDYFEWLE-amide as substrate preincubated for 5 to 10 mins followed by substrate addition and measured after 1 hr by HTRF assay
    [PMID: 36356320]
    体外実験

    Cells expressing the FGFR2-CLIP1 fusion is sensitive to Pemigatinib (INCB054828; IC50 value 10.16 nM), while cells with added N549H mutation is resistant to Pemigatinib (IC50 value of 1527.57 nM)[3].

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

    臨床実験
    分子量

    487.50

    分子式

    C24H27F2N5O4

    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    CCN(C(N(C(C(F)=C(OC)C=C1OC)=C1F)C2)=O)C(C2=CN3)=C4C3=NC(CN5CCOCC5)=C4

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 25 mg/mL (51.28 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 2.0513 mL 10.2564 mL 20.5128 mL
    5 mM 0.4103 mL 2.0513 mL 4.1026 mL
    10 mM 0.2051 mL 1.0256 mL 2.0513 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    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:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (5.64 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (4.27 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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
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    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.
    純度とドキュメンテーション

    純度: 99.84%

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0513 mL 10.2564 mL 20.5128 mL 51.2821 mL
    5 mM 0.4103 mL 2.0513 mL 4.1026 mL 10.2564 mL
    10 mM 0.2051 mL 1.0256 mL 2.0513 mL 5.1282 mL
    15 mM 0.1368 mL 0.6838 mL 1.3675 mL 3.4188 mL
    20 mM 0.1026 mL 0.5128 mL 1.0256 mL 2.5641 mL
    25 mM 0.0821 mL 0.4103 mL 0.8205 mL 2.0513 mL
    30 mM 0.0684 mL 0.3419 mL 0.6838 mL 1.7094 mL
    40 mM 0.0513 mL 0.2564 mL 0.5128 mL 1.2821 mL
    50 mM 0.0410 mL 0.2051 mL 0.4103 mL 1.0256 mL
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    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
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    製品名:
    Pemigatinib
    製品番号:
    HY-109099
    数量:
    MCE 日本正規代理店: