2. Protein Tyrosine Kinase/RTK
  3. FGFR
  4. Fexagratinib

Fexagratinib  (Synonyms: AZD4547; ADSK091)

Cat. No.: HY-13330 Purity: 99.85%
COA Handling Instructions

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Fexagratinib (AZD4547; ADSK091) is a potent inhibitor of the FGFR family with IC50s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

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

Fexagratinib Chemical Structure

Fexagratinib Chemical Structure

CAS No. : 1035270-39-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 92 In-stock
50 mg USD 185 In-stock
100 mg USD 251 In-stock
200 mg USD 356 In-stock
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Customer Review

Based on 24 publication(s) in Google Scholar

Fexagratinib Related Antibodies

Top Publications Citing Use of Products

    Fexagratinib purchased from MedChemExpress. Usage Cited in: Front Cell Dev Biol. 2020 May 7;8:287.  [Abstract]

    Determination in L3.6 cells of FGF2-induced FGFR phosphorylation by Western blot in the presence of AZD4547 . FGFR1 and alpha-Tubulin are used as loading controls.

    View All FGFR Isoform Specific Products:

    View All Isoforms
    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fexagratinib (AZD4547; ADSK091) is a potent inhibitor of the FGFR family with IC50s of 0.2 nM, 2.5 nM, 1.8 nM, and 165 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.

    IC50 & Target[1]

    FGFR1

    0.2 nM (IC50)

    FGFR2

    2.5 nM (IC50)

    FGFR3

    1.8 nM (IC50)

    FGFR4

    165 nM (IC50)

    In Vitro

    Fexagratinib also inhibits recombinant VEGFR2 (KDR) kinase activity with an IC50 of 24 nM. In KG1a, Sum52-PE, MCF7, and KMS11 cell lines, Fexagratinib potently inhibits autophosphorylation of FGFR1, 2, and 3 tyrosine kinases (IC50 values of 12, 2, and 40 nM, respectively) and displays weaker inhibition of FGFR4 cellular kinase activity (IC50=142 nM). Significantly weaker inhibitory activity is observed versus cellular KDR and IGFR ligand-induced phosphorylation (IC50 values of 258 and 828 nM, respectively), representing approximately 20- and 70-fold selectivity over cellular FGFR1. Besides, Fexagratinib potently inhibits FGFR phosphorylation and downstream signaling affected through FRS2, PLCγ, and MAPK at the cellular level[1].

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

    Fexagratinib Related Antibodies
    In Vivo

    Female SCID mice bearing KMS11 tumors are randomized and treated chronically with Fexagratinib at a range of well-tolerated doses. Oral Fexagratinib treatment results in dose-dependent tumor growth inhibition. Twice daily administration of Fexagratinib at 3 mg/kg gives statistically significant tumor growth inhibition of 53% (P<0.0005 by one-tailed t test) when compare with vehicle-treated controls, whereas doses of 12.5 mg/kg once daily and 6.25 mg/kg twice daily results in complete tumor stasis (P<0.0001). A further efficacy study in the KG1a model with 12.5 mg/kg once daily Fexagratinib results in 65% tumor growth inhibition (P=0.002)[1].

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

    463.57

    Formula

    C26H33N5O3
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    C[C@H](C1)N[C@@H](C)CN1C2=CC=C(C(NC3=NNC(CCC4=CC(OC)=CC(OC)=C4)=C3)=O)C=C2
    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 : 125 mg/mL (269.65 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 2.1572 mL 10.7859 mL 21.5717 mL
    5 mM 0.4314 mL 2.1572 mL 4.3143 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)

    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 (5.39 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: ≥ 2.08 mg/mL (4.49 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  1% CMC-Na/saline water

      Solubility: 3.33 mg/mL (7.18 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

    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).
    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: 99.85%

    COA (251 KB) LCMS (265 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    Cell lines are incubated with fixed concentrations of AZD4547 for 72 hours. For fluorescence-activated cell sorting (FACS), cells are fixed with 70% ethanol and then incubated with propidium iodide/RNase A labeling solution. Cell-cycle profiles are assessed with a FACSCalibur instrument and CellQuest analysis software. For apoptotic analysis, cells and media are gently harvested and centrifuged, followed by washing of cell pellets. Cells are then processed for FITC staining and propidium iodide uptake. The proportion of cells staining positive for Annexin V are then assessed with a FACSCalibur instrument and quadrant sorting is done by CellQuest analysis software[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Mice[1]
    Swiss derived nude (nu/nu) and severe combined immunodeficient mice (SCID) are used. Tumor xenografts are established by s.c. injection into the left flank with 0.1 mL tumor cells (1×106 for LoVo, 1×107 for HCT-15, and 1×107 for Calu-6) or 0.2 mL (2×107 for KMS11 and KG1a) mixed 1:1 with Matrigel, with the exception of LoVo and HCT-15, which do not include Matrigel. Mice are randomized into control and treatment groups (AZD4547, 1.5-50 mg/kg, once daily or twice daily by oral gavage) when tumors reach the determined size of more than 0.2 cm3. Tumor volume (measured by caliper), animal body weight, and tumor condition are recorded twice weekly for the duration of the study. Tumor volume is calculated.

    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 2.1572 mL 10.7859 mL 21.5717 mL 53.9293 mL
    5 mM 0.4314 mL 2.1572 mL 4.3143 mL 10.7859 mL
    10 mM 0.2157 mL 1.0786 mL 2.1572 mL 5.3929 mL
    15 mM 0.1438 mL 0.7191 mL 1.4381 mL 3.5953 mL
    20 mM 0.1079 mL 0.5393 mL 1.0786 mL 2.6965 mL
    25 mM 0.0863 mL 0.4314 mL 0.8629 mL 2.1572 mL
    30 mM 0.0719 mL 0.3595 mL 0.7191 mL 1.7976 mL
    40 mM 0.0539 mL 0.2696 mL 0.5393 mL 1.3482 mL
    50 mM 0.0431 mL 0.2157 mL 0.4314 mL 1.0786 mL
    60 mM 0.0360 mL 0.1798 mL 0.3595 mL 0.8988 mL
    80 mM 0.0270 mL 0.1348 mL 0.2696 mL 0.6741 mL
    100 mM 0.0216 mL 0.1079 mL 0.2157 mL 0.5393 mL
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    Fexagratinib 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:

    Fexagratinib1035270-39-3AZD4547 ADSK091AZD 4547AZD-4547ADSK091ADSK 091ADSK-091FGFRFibroblast growth factor receptorInhibitorinhibitorinhibit

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