2. Protein Tyrosine Kinase/RTK
  3. VEGFR FGFR PDGFR
  4. SU 5402

SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.

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

CAS No. : 215543-92-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of SU 5402:

SU 5402 Related Antibodies

Top Publications Citing Use of Products

    SU 5402 purchased from MedChemExpress. Usage Cited in: EMBO J. 2025 Nov 24.  [Abstract]

    WISH of tbxta, cdx4 in Bmp4 explants treated with Nodal inhibitor (SB505124, 50 μM), Wnt inhibitor (IWP-L6, 25 μM) or SU 5402 (25 μM) at 6 hpf, with injection sites oriented to the right. Representative images of treated or untreated Bmp4 explants at 24 hpf are displayed.

    SU 5402 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2025 Jul 30;26(15):7361.  [Abstract]

    The FGFR inhibitor SU 5402 (20 μM) reduced the expression of the repellent factor Slit1.

    SU 5402 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 Apr 9;25(8):4138.

    SU 5402 (10 μM; 4 d). Brightfield indicated the cell morphology and immunostaining of markers for NNE, stemness and PPE on day 4 of differentiation. The change in cell morphology and immunostaining of the NNE marker TFAP2A (red), the stemness marker OCT4 (red), and the PPE marker SIX1 (green) were also indicated. Arrows indicated SIX1+ cells.

    SU 5402 purchased from MedChemExpress. Usage Cited in: J Hazard Mater. 2020 Jul 5;393:122440.  [Abstract]

    Shown are the qRT-PCR analyses for the expression of FGF related genes, after treatment with SU 5402 (30 nM) and 0.1 μg/mL AgNPs or AgNO3, for 12 days during the differentiation.

    SU 5402 purchased from MedChemExpress. Usage Cited in: Theriogenology. 2019 Nov:139:90-97.  [Abstract]

    Effect of bFGF and SU5402 on BrdU incorporation in proliferating cells and TUNEL labeling of the apoptotic cells. Red fluorescence: BrdU-labelled cells, mainly distributed in the follicular theca externa. Green fluorescence: TUNEL -labelled cells. Blue fluorescence: DAPI staining. DeE: The percentage of BrdU-positive cells and TUNEL-positive cells. SU 5402 blocks the ability of bFGF to significantly increase the ratio of BrdU-labelled cells. The opposite situation was observed in the results of TUNEL assay.

    View All VEGFR Isoform Specific Products:

    View All Isoforms
    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

    View All PDGFR Isoform Specific Products:

    View All Isoforms
    PDGFR PDGFRβ PDGFRα

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    SU 5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGFRβ, respectively.

    IC50 & Target[1]

    VEGFR2

    20 nM (IC50)

    FGFR1

    30 nM (IC50)

    PDGFRβ

    510 nM (IC50)

    Cellular Effect
    Cell Line Type Value Description References
    HUVEC IC50
    0.05 μM
    Compound: 2
    Evaluated for the inhibition of cell proliferation induced by VEGF in HUVEC or NIH3T3 cells
    Evaluated for the inhibition of cell proliferation induced by VEGF in HUVEC or NIH3T3 cells
    		[PMID: 10893303]
    HUVEC IC50
    2.8 μM
    Compound: 2
    Evaluated for the inhibition of cell proliferation induced by FGF in HUVEC or NIH3T3 cells
    Evaluated for the inhibition of cell proliferation induced by FGF in HUVEC or NIH3T3 cells
    		[PMID: 10893303]
    HUVEC IC50
    28.4 μM
    Compound: 2
    Evaluated for the inhibition of cell proliferation induced by PDGF in HUVEC or NIH3T3 cells
    Evaluated for the inhibition of cell proliferation induced by PDGF in HUVEC or NIH3T3 cells
    		[PMID: 10893303]
    HUVEC IC50
    > 50 μM
    Compound: 2
    Evaluated for the inhibition of cell proliferation induced by EGF in HUVEC or NIH3T3 cells
    Evaluated for the inhibition of cell proliferation induced by EGF in HUVEC or NIH3T3 cells
    		[PMID: 10893303]
    NIH3T3 IC50
    10 μM
    Compound: SU-5402
    Inhibition of acidic FGF-stimulated FGFR1 tyrosine autophosphorylation in mouse NIH/3T3 cells by immunoblotting
    Inhibition of acidic FGF-stimulated FGFR1 tyrosine autophosphorylation in mouse NIH/3T3 cells by immunoblotting
    		[PMID: 9139660]
    In Vitro

    SU 5402 is cocrystallized with the catalytic domain of FGF-R1 (flg-1) and is found to inhibit tyrosine phosphorylation of VEGF-R2 (Flk-1/KDR) and PDGF-R in NIH 3T3 cells with IC50 values of 0.4 and 60.9 μM, respectively[1]. In order to investigate whether phosphorylation of PKM2 and LDHA is mediated in FGFR1-specific manner, FTC-133 are treated with receptor tyrosine kinase inhibitors Dovitinib and SU 5402 (SU-5402). Dovitinib treatment results in significant decrease of phosphorylation status at a concentration of 100 nM after four hours of incubation for both PKM2 and LDHA. No significant changes are seen when administered at concentrations of 1 nM and 10 nM. SU 5402 administration leads to a sigificant decrease of PKM2 and LDHA phosphorylation at a concentration of 20 μM[2].

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

    SU 5402 Related Antibodies
    In Vivo

    Inhibition of FGFR1 with SU 5402 (SU5402) administered to ΔF508-CFTR homozygous mice results in partial ΔF508-CFTR rescue, as shown by an increase in saliva secretion, a surrogate "sweat test" assay in mice. As salivary secretion is often sex dependent, only male mice are chosen for these experiments. Our results indicate that treatment of the ΔF508-CFTR mice with SU 5402 restores the saliva secretion level to ~10% of that observed for the wild-type CFTR mice, which suggests that SU 5402 can have therapeutic benefits to Cystic Fibrosis (CF)[3]. The selective FGFR1 inhibitor SU 5402 (SU5402) prevents and/or reverses PH induced by MCT (monocrotaline) in rats. In rats treated with SU 5402 on days 21 to 42 after the MCT injection, evaluations on day 42 show marked decreases in pulmonary artery pressure (PAP), RV/(LV+S), and distal artery muscularization compare with rats treated with the vehicle (saline)[4].

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

    296.32

    Formula

    C17H16N2O3
    CAS No.
    Appearance

    Solid

    Color

    Light brown to orange

    SMILES

    O=C(CCC1=C(NC=C1C)/C=C2C(NC3=C\2C=CC=C3)=O)O
    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 : ≥ 30 mg/mL (101.24 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.3747 mL 16.8736 mL 33.7473 mL
    5 mM 0.6749 mL 3.3747 mL 6.7495 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

    V1

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    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 (8.44 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.
    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
    References
    Cell Assay
    [2]

    8505C and FTC133 cells are grown in DMEM/F12 suppplemented with 10% FCS and 1% PenStrep and incubated at 37°C, 5% CO2. For B-CPAP RPMI 1640 medium is used. FGFR1 inhibition experiments are performed on FTC133 cells by employment of Receptor Tyrosine Kinase Inhibitors TKI-258 (Dovitinib) and SU 5402 (20μM). Inhibition is conducted over 4 h with the indicated inhibitor concentrations. Control cells receive corresponding concentrations of DMSO[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3][4]

    Mice[3]
    Male ΔF508 mice (CFTRtm1Eur on a 129/FVB background) and their wild-type littermates of 9-12 weeks are intraperitoneally injected with DMSO or SU 5402 (dissolved in DMSO at the concentration of 6 mg/mL) at 25 mg/kg body weight, every day for 1 week. The mice are weighed daily and the dosages adjusted accordingly. The mice are then anesthetized by inhaling isoflurane until the end of the procedure. Cholinergic antagonist, Atropine (1 mM, 50 μL) is subcutaneously injected into the right cheek to block potential cholinergic stimulation of the salivary gland. A small strip of filter paper is placed against the injected cheek, for 4 min. Isoprenaline (10 mM, 37.5 μL) is subsequently injected in the same spot to stimulate an adrenergic secretion of saliva (time 0). Filter strips (pre-weighed in an Eppendorf tube) are replaced every 5 min, over a period of 30 min. All six filter strips are weighed at the end of the collection and the results are normalized relative to mg/g body weight.
    Rats[4]
    To assess the potential effects of the FGFR1 inhibitor SU 5402 on established PH, adult male Wistar rats (200-250 g) are given MCT (60 mg/kg s.c.), left untreated for 21 days, then randomly divided into 2 groups (10 animals in each group), of which one is treated with SU 5402 (25 mg/kg/day) and the other given the vehicle, from day 21 to day 42. All treatments are given once a day by s.c. injection.

    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, 6 months; -20°C, 1 month. 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 3.3747 mL 16.8736 mL 33.7473 mL 84.3682 mL
    5 mM 0.6749 mL 3.3747 mL 6.7495 mL 16.8736 mL
    10 mM 0.3375 mL 1.6874 mL 3.3747 mL 8.4368 mL
    15 mM 0.2250 mL 1.1249 mL 2.2498 mL 5.6245 mL
    20 mM 0.1687 mL 0.8437 mL 1.6874 mL 4.2184 mL
    25 mM 0.1350 mL 0.6749 mL 1.3499 mL 3.3747 mL
    30 mM 0.1125 mL 0.5625 mL 1.1249 mL 2.8123 mL
    40 mM 0.0844 mL 0.4218 mL 0.8437 mL 2.1092 mL
    50 mM 0.0675 mL 0.3375 mL 0.6749 mL 1.6874 mL
    60 mM 0.0562 mL 0.2812 mL 0.5625 mL 1.4061 mL
    80 mM 0.0422 mL 0.2109 mL 0.4218 mL 1.0546 mL
    100 mM 0.0337 mL 0.1687 mL 0.3375 mL 0.8437 mL
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    SU 5402 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:

    SU 5402215543-92-3SU5402SU-5402VEGFRFGFRPDGFRVascular endothelial growth factor receptorFibroblast growth factor receptorPlatelet-derived growth factor receptorInhibitorinhibitorinhibit

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