1. Protein Tyrosine Kinase/RTK Apoptosis
  2. FGFR Apoptosis
  3. Erdafitinib

Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

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

CAS No. : 1346242-81-6

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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Erdafitinib:

Top Publications Citing Use of Products

39 Publications Citing Use of MCE Erdafitinib

Cell Proliferation/Viability Assay
In Vivo Efficacy Study
WB
RT-PCR
IHC

    Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24.  [Abstract]

    C, Cell Counting Kit-8 assay revealed the cell viability of WT and SRM KO MGH-U3 cells treated with erdafitinib (10 or 100 nmol/L; 24-96 h) or DMSO.

    Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24.  [Abstract]

    formed by subcutaneous injection of WT and SRM KO MGH-U3 cells into the right flanks of nude mice treated with DMSO or erdafitinib (5 or 15 mg/kg)

    Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24.  [Abstract]

    Western blotting with the indicated antibodies in WT and SRM KO MGH-U3 cells treated with 10 or 100 nmol/L erdafitinib and DMSO for 96 hours.

    Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24.  [Abstract]

    The expression of EGFR was detected by qRT-PCR in WT and SRM KO MGH-U3 cells treated with 100 nmol/L erdafitinib for 96 hours.

    Erdafitinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Mar 24.  [Abstract]

    Mice were treated with DMSO, 5 mg/kg afatinib, 15 mg/kg erdafitinib, or combinational treatment. IHC staining of Ki67 on WT MGH-U3 xenografts was performed as in vivo.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.

    IC50 & Target[1]

    FGFR1

    1.2 nM (IC50)

    FGFR2

    2.5 nM (IC50)

    FGFR3

    3.0 nM (IC50)

    FGFR4

    5.7 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    A2780 IC50
    0.02 μM
    Compound: 1; JNJ-42756493
    Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A2780 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 36449947]
    A2780 IC50
    0.02 μM
    Compound: Erdafitnib
    Antiproliferative activity against human A2780 cells
    Antiproliferative activity against human A2780 cells
    [PMID: 38964169]
    AN3-CA GI50
    0.048 μM
    Compound: 2
    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: 2
    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
    0.761 μM
    Compound: 2
    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
    4.011 μM
    Compound: 2
    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
    > 300 nM
    Compound: 1
    Growth inhibition against mouse BaF3 cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against mouse BaF3 cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    BaF3 GI50
    > 5 μM
    Compound: 2
    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: 2
    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]
    BaF3 IC50
    0.1 nM
    Compound: 5
    Inhibition of VEGFR2 in mouse BAF3 cells
    Inhibition of VEGFR2 in mouse BAF3 cells
    10.1039/C9MD90044F
    DMS-114 IC50
    11 nM
    Compound: 1
    Inhibition of cell viability in human DMS-114 cells harboring FGFR1-amplification incubated for 72 to 120 hrs by Cell Titer Glo assay
    Inhibition of cell viability in human DMS-114 cells harboring FGFR1-amplification incubated for 72 to 120 hrs by Cell Titer Glo assay
    [PMID: 39258897]
    HCT-116 IC50
    4.24 μM
    Compound: 1; JNJ-42756493
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 36449947]
    HCT-116 IC50
    4.24 μM
    Compound: Erdafitnib
    Antiproliferative activity against human HCT-116 cells
    Antiproliferative activity against human HCT-116 cells
    [PMID: 38964169]
    J82 GI50
    3.796 μM
    Compound: 2
    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]
    Jurkat IC50
    6.81 μM
    Compound: 1; JNJ-42756493
    Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human Jurkat cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 36449947]
    Jurkat IC50
    6.81 μM
    Compound: Erdafitnib
    Antiproliferative activity against human Jurkat cells
    Antiproliferative activity against human Jurkat cells
    [PMID: 38964169]
    K562 GI50
    > 300 nM
    Compound: 1
    Growth inhibition against human K562 cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against human K562 cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    K562 IC50
    3.02 μM
    Compound: 1; JNJ-42756493
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 36449947]
    K562 IC50
    3.02 μM
    Compound: Erdafitnib
    Antiproliferative activity against human K562 cells
    Antiproliferative activity against human K562 cells
    [PMID: 38964169]
    KG-1 IC50
    2.1 nM
    Compound: 1
    Inhibition of cell viability in human KG-1 cells harboring FGFR1-fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
    Inhibition of cell viability in human KG-1 cells harboring FGFR1-fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
    [PMID: 39258897]
    KG-1a GI50
    5 nM
    Compound: 1
    Growth inhibition against human KG-1a cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against human KG-1a cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    KMS-11 GI50
    0.39 μM
    Compound: 2
    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]
    KMS-11 GI50
    150 nM
    Compound: 1
    Growth inhibition against human KMS-11 cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against human KMS-11 cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    MDA-MB-453 GI50
    44 nM
    Compound: 1
    Growth inhibition against human MDA-MB-453 cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against human MDA-MB-453 cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    MFE-296 GI50
    41 nM
    Compound: 1
    Growth inhibition against human MFE-296 cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against human MFE-296 cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    NCI-H716 GI50
    0.9 nM
    Compound: 1
    Growth inhibition against human NCI-H716 cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against human NCI-H716 cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    RT-112 IC50
    1.3 nM
    Compound: Erdafitinib
    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
    107 nM
    Compound: Erdafitinib
    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
    2.4 nM
    Compound: Erdafitinib
    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
    39 nM
    Compound: Erdafitinib
    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
    603 nM
    Compound: Erdafitinib
    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]
    RT-4 GI50
    < 10 nM
    Compound: 1
    Growth inhibition against human RT-4 cells incubated for 72 to 96 hrs by MTT assay
    Growth inhibition against human RT-4 cells incubated for 72 to 96 hrs by MTT assay
    [PMID: 38294952]
    RT-4 IC50
    4.4 nM
    Compound: 1
    Inhibition of cell viability in human RT-4 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
    Inhibition of cell viability in human RT-4 cells harboring FGFR3/TACC3 fusion incubated for 72 to 120 hrs by Cell Titer Glo assay
    [PMID: 39258897]
    SNU-16 IC50
    0.0007 μM
    Compound: 1; JNJ-42756493
    Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human SNU-16 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 36449947]
    SNU-16 IC50
    0.7 nM
    Compound: Erdafitnib
    Antiproliferative activity against human SNU-16 cells
    Antiproliferative activity against human SNU-16 cells
    [PMID: 38964169]
    SNU-16 IC50
    2.7 nM
    Compound: Erdafitinib
    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]
    Sf21 IC50
    3 nM
    Compound: JNJ-42756493
    Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved fluorescence assay
    Inhibition of human recombinant N-terminal His6 tagged FGFR3 (447 to 761 residues) expressed in Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition measured after 60 mins in presence of ATP by time resolved fluorescence assay
    [PMID: 32278710]
    Sf21 IC50
    36.8 nM
    Compound: JNJ-42756493
    Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence assay
    Inhibition of human N-terminal His6-tagged VEGFR2 (790 to end residues) expressed in baculovirus infected Sf21 cells using FLT3 peptide as substrate preincubated for 60 mins followed by substrate addition in presence of ATP by time resolved fluorescence assay
    [PMID: 32278710]
    Sf9 IC50
    0.003 μM
    Compound: 5
    Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA
    Inhibition of wild type His-tagged human FGFR3 (455 to 763 residues) expressed in Sf9 insect cells by ELISA
    10.1039/C9MD90044F
    In Vitro

    Erdafitinib (JNJ-42756493) inhibits the tyrosine kinase activities of FGFR1-4 in time-resolved fluorescence assays with IC50 values of 1.2, 2.5, 3.0 and 5.7 nM, respectively. The closely related VEGFR2 kinase is less potently inhibited (30-fold less potent compared to FGFR1) by erdafitinib, with an IC50 value of 36.8 nM. Erdafitinib binds FGFR1, 3, 4, and 2 with Kd values of 0.24, 1.1, 1.4 and 2.2 nM, respectively. The Kd value for VEGFR2 is higher at 6.6 nM. Erdafitinib inhibits proliferation of FGFR1, 3, and 4 expressing cells with IC50 values of 22.1, 13.2, and 25nM, respectively[1].

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

    In Vivo

    In xenografts from human tumor cell lines or patient-derived tumor tissue with activating FGFR alterations, Erdafitinib administration results in potent and dose-dependent antitumor activity accompanied by pharmacodynamic modulation of phospho-FGFR and phospho-ERK in tumors[1].

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

    Clinical Trial
    Molecular Weight

    446.54

    Formula

    C25H30N6O2

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    CN1N=CC(C2=NC3=CC(N(C4=CC(OC)=CC(OC)=C4)CCNC(C)C)=CC=C3N=C2)=C1

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 62.5 mg/mL (139.97 mM; Need ultrasonic; 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 2.2394 mL 11.1972 mL 22.3944 mL
    5 mM 0.4479 mL 2.2394 mL 4.4789 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 2.75 mg/mL (6.16 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.75 mg/mL (6.16 mM); Clear solution

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    (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:
    %
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    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: 99.66%

    References
    Cell Assay
    [1]

    Erdafitinib is dissolved in DMSO. KATO III, RT-112, A-204, RT-4, DMS-114, A-427 and MDA-MB-453 cells are treated with erdafitinib (from 10 μM to 0.01 nM in 2% DMSO, final concentration). Following 4-day incubation, cell viability is determined using MTT reagent. The optical density is determined at 540 nm[1].

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

    Animal Administration
    [1]

    Mice: Mice bearing SNU-16 human gastric carcinoma (FGFR2 amplified) xenograft tumors are dosed orally with 0, 3, 10 or 30 mg/kg Erdafitinib. Tumor tissue and mouse plasma (3 mice per time point) are harvested at 0.5, 1, 3, 7, 16 and 24h post-dosing[1].

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

    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, 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 2.2394 mL 11.1972 mL 22.3944 mL 55.9860 mL
    5 mM 0.4479 mL 2.2394 mL 4.4789 mL 11.1972 mL
    10 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5986 mL
    15 mM 0.1493 mL 0.7465 mL 1.4930 mL 3.7324 mL
    20 mM 0.1120 mL 0.5599 mL 1.1197 mL 2.7993 mL
    25 mM 0.0896 mL 0.4479 mL 0.8958 mL 2.2394 mL
    30 mM 0.0746 mL 0.3732 mL 0.7465 mL 1.8662 mL
    40 mM 0.0560 mL 0.2799 mL 0.5599 mL 1.3997 mL
    50 mM 0.0448 mL 0.2239 mL 0.4479 mL 1.1197 mL
    60 mM 0.0373 mL 0.1866 mL 0.3732 mL 0.9331 mL
    80 mM 0.0280 mL 0.1400 mL 0.2799 mL 0.6998 mL
    100 mM 0.0224 mL 0.1120 mL 0.2239 mL 0.5599 mL
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