1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. Semaxinib

Semaxinib (SU5416) est un inhibiteur de VEGFR (Flk-1/KDR) qui est puissant et sélectif avec un IC50 de 1,23 μM.

Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC50 of 1.23 μM.

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

Semaxinib Chemical Structure

Semaxinib Chemical Structure

CAS No. : 204005-46-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 36 publication(s) in Google Scholar

Other Forms of Semaxinib:

Top Publications Citing Use of Products

35 Publications Citing Use of MCE Semaxinib

WB

    Semaxinib purchased from MedChemExpress. Usage Cited in: BMC Anesthesiol. 2019 Jul 9;19(1):127.  [Abstract]

    The hCMEC/D3 cells are incubated with TNF-α and VEGFR-2 inhibitor (SU5416, 10 μM). Left side shows the image of a representative Western blot for VEGF, p-VEGFR-2, p-ERK, ERK and occludin in hCMEC/D3 cells. Right side is the plot of normalized ratios of optical densities. β-actin is served as internal loading control.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Semaxinib (SU5416) is a potent and selective inhibitor of VEGFR (Flk-1/KDR) with an IC50 of 1.23 μM[1].

    IC50 & Target[1]

    Flk-1

    1.23 μM (IC50)

    In Vitro

    Semaxinib (SU5416) inhibits VEGF-driven mitogenesis in a dose-dependent manner with an IC50 of 0.04±0.02 μM (n=3). In contrast, Semaxinib (SU5416) blocks FGF-dependent mitogenesis of HUVECs with an IC50 of 50 μM (n=10). An IC50 of 20.26±5.2 μM, which is about 20-fold less in potency on PDGF-dependent autophosphorylation, is observed when SU5416 is tested in NIH 3T3 cells overexpressing the human PDGF receptor β[1].

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

    In Vivo

    Daily administration of Semaxinib (SU5416) (i.p., 3 mg/kg/day) inhibits the local growth of C6 tumors in the colon. A comparable level of growth inhibition (62% by day 16; P=0.001) is observed for tumors growing in the colon in comparison with ones growing in the hindflank region (54% by day 18; P=0.001). These results indicate that Semaxinib (SU5416) could inhibit tumor growth at a site other than the subcutaneous implantation site, where the preexisting vasculature may be different[1]. Daily treatment with Semaxinib (SU5416) (25 mg/kg) results in a significantly lower tumor growth rate with tumor masses of up to 8% of that present in control animals by day 22 after implantation. Inhibition of tumor growth is clearly preceded by a marked reduction of the tissue area covered by the newly formed glioma microvasculature in the Semaxinib-treated group, indicating a reduced initial tumor vascularization[2].

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

    Clinical Trial
    Molecular Weight

    238.28

    Formula

    C15H14N2O

    CAS No.
    Appearance

    Solid

    Color

    Brown to orange

    SMILES

    O=C(NC1=CC=CC=C/21)C2=C/C3=C(C)C=C(C)N3

    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: 

    DMF : 50 mg/mL (209.84 mM; Need ultrasonic)

    DMSO : 20 mg/mL (83.93 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 4.1967 mL 20.9837 mL 41.9674 mL
    5 mM 0.8393 mL 4.1967 mL 8.3935 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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    Volume (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:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (10.49 mM); Suspended solution

      This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

      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.
    • Protocol 2

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

      Solubility: 2.25 mg/mL (9.44 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.25 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 (22.5 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)

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    Dosing volume
    (per animal)

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    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: 99.96%

    References
    Cell Assay

    3T3Her2 and 488G2M2 are NIH3T3 fibroblast cell lines engineered to overexpress Her2 and to express human PDGF-BB and human PDGF receptor β. Both cell lines are cultured in DMEM supplemented with 2% CS and 2 mM L-glutamine. C6, Calu 6, A375, A431, and SF767T are plated in their respective growth medium at 2×103 cells/100 μL/well in 96-well, flat-bottomed plates. Semaxinib (SU5416) is serially diluted in media containing DMSO (<0.5%) and added to cultures of tumor cells 1 day after the initiation of culture. Cell growth is measured after 96 h using the sulforhodamine B method. IC50s are calculated by curve fitting using four-parameter analysis[1].

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

    Animal Administration
    [1][3]

    Mice[1]
    Female BALB/c nu/nu mice (20-22 g; 12 weeks of age) are used. Aseptic technique is used during this surgical procedure. A small midline incision (1 cm) is made in the abdomen directly over the colon. C6 cells are implanted (0.5×106 cells/animal) under the serosa of the colon using a 27-gauge needle. After implantation, all exposed sections of the intestine are returned into the abdominal cavity. The peritoneum and skin are closed using a 6.0 surgical suture and wound clips. The wound clips are removed 7 days after surgery. Animals are treated once daily with a 50 μL i.p. bolus injection of either Semaxinib (SU5416) or DMSO, beginning 1 day after implantation. Approximately 13-16 days after implantation, animals are euthanized, and local tumor growth on the colon is quantitated either by weighing the tumors or by measuring the tumors using venier calipers. Tumor volumes are calculated as the product of length×width×height.
    Rats[3]
    Male Sprague Dawley rats (n=60, 6-8 wk) are randomly divided among five groups: control (Con), Semaxinib (SU), pneumonectomy (PNx), Semaxinib+hypoxia (SuHx), and Semaxinib+PNx (SuPNx). The SuHx protocol is employed. Briefly, animals are injected with Semaxinib (25 mg/kg) dissolved in carboxymethylcellulose (CMC) and exposed to hypoxia (10%) for 4 wk followed by re-exposure to normoxia. PNx animals underwent a left pneumonectomy. Two days following PNx surgery an injection of Semaxinib is administered (25 mg/kg). The Con group received only the solvent CMC. Echocardiography is utilized at baseline (prehypoxia/presurgery), week 2, and week 6 to determine cardiac morphometry and function. Two and six weeks postsurgery/posthypoxia animals are anesthetized and right ventricle (RV) and left ventricle (LV) pressure measurements via catheterization are performed.

    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 / DMF 1 mM 4.1967 mL 20.9837 mL 41.9674 mL 104.9186 mL
    5 mM 0.8393 mL 4.1967 mL 8.3935 mL 20.9837 mL
    10 mM 0.4197 mL 2.0984 mL 4.1967 mL 10.4919 mL
    15 mM 0.2798 mL 1.3989 mL 2.7978 mL 6.9946 mL
    20 mM 0.2098 mL 1.0492 mL 2.0984 mL 5.2459 mL
    25 mM 0.1679 mL 0.8393 mL 1.6787 mL 4.1967 mL
    30 mM 0.1399 mL 0.6995 mL 1.3989 mL 3.4973 mL
    40 mM 0.1049 mL 0.5246 mL 1.0492 mL 2.6230 mL
    50 mM 0.0839 mL 0.4197 mL 0.8393 mL 2.0984 mL
    60 mM 0.0699 mL 0.3497 mL 0.6995 mL 1.7486 mL
    80 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3115 mL
    DMF 100 mM 0.0420 mL 0.2098 mL 0.4197 mL 1.0492 mL
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    • 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.

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