Semaxanib (SU5416)

Catalog No.S2845

Semaxanib (SU5416) Chemical Structure

Molecular Weight(MW): 238.28

Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.

Size Price Stock Quantity  
In DMSO USD 200 In stock
USD 170 In stock
USD 270 In stock
USD 970 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

  • Injected tumor cells move to the tail via blood vessels. Tg (flil1:egfp) embryos at 20 hpf were treated with 2 μM SU5416 for 1 hr (+SU5416) to inhibit vasculogenesis24; the control fish were treated with 0.02% DMSO for 1 hr (-SU5416). After 1 hr, SU5416 or DMSO was washed out by changing fish media. At 48 hpf, tfRFP-B16 cells were injected into the pericardium cavity of fish. Representative images show that tumor cells moved to the tail in a drug-free larva, while no tumor cells moved to the tail in a drug-treated larva after new vessels were inhibited by SU5416. Insets are enlarged images from each corresponding tip of the tail indicated by white arrows. Dashed white lines mark extravasated tumor cells at 12 hpi. Vessels are green and tumor cells are red. –SU5416, 6 other larvae exhibit similar behaviors; +SU5416, 3 other larvae exhibit similar behaviors. Scale bars, 500 μm. Insets, 100 μm.

    Sci Rep, 2016, 6:19304. . Semaxanib (SU5416) purchased from Selleck.

Purity & Quality Control

Choose Selective VEGFR Inhibitors

Biological Activity

Description Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.
VEGFR2/Flk1 [1]
(Cell-free assay)
1.23 μM
In vitro

Semaxanib inhibits VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with IC50 of 1.04 μM. Semaxanib inhibits PDGF-dependent autophosphorylation in NIH 3T3 cells with IC50 of 20.3 μM. Semaxanib inhibits VEGF- and FGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 and 50 μM, respectively. Semaxanib treatment has no effect on the in vitro growth of C6 glioma, Calu 6 lung carcinoma, A375 melanoma, A431 epidermoid carcinoma, and SF767T glioma cells (all IC50s > 20 μM). [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells MWHDfZRwfG:6aXPpeJkh[XO|YYm= MlnNOFghcA>? MUTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDDR2s5KGG|c3H5MEBKSzVyPUOuNUBvVQ>? MUKyN|c4Pzh7OB?=
mouse B16F10 cells MmLzR5l1d3SxeHnjbZR6KGG|c3H5 NEnHNYo1QCCq MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCNVZHOTBiY3XscJMh[W[2ZYKgOFghcHK|IHL5JGNEUzhiYYPzZZktKEmFNUC9N{43KG6P NUHlXHA3OjN5N{e4PVg>
human U251 cells M3ezeGZ2dmO2aX;uJIF{e2G7 MoqwTY5pcWKrdHnvckBw\iCYRVfGVlIhcW5iaIXtZY4hXTJ3MTDj[YxteyCkeTDwbI9{eGixdInyc5NqdmViRVzJV2EtKEmFNUC9NVIvQSCwTR?= MWGyOFkxODh4NR?=
human A431 cells MUDGeY5kfGmxbjDhd5NigQ>? M3TRNmFvfGmjbnfpc4dmdmmlIHHjeIl3cXS7IHHnZYlve3RiaIXtZY4hSTR|MTDj[YxteyxiSVO1NF0xNjB6NTFOwG0> NWLadHRMOjB2MEO2PVM>
CHO cells NFvqOYFHfW6ldHnvckBie3OjeR?= MnHqTY5pcWKrdHnvckBw\iCYRVfGVkBqdmS3Y3XkJIF2fG:yaH;zdIhwenmuYYTpc44hd2ZiaIXtZY4hXmG|Y4XsZZIh\W6mb4To[Yxq[WxiZ4Lve5RpKG[jY4TvdkBz\WOncITvdkAzKCiYRVfGVlIqKHS{YX7z[oVkfGWmIHnuJGNJVyClZXzsd{whUUN3ME2wMlg5PCEQvF2= NYm2dmFQOTJ2N{ezOVI>
human MCF7 cells MUTQdo9tcW[ncnH0bY9vKGG|c3H5 M3i2O|Qh\GG7cx?= NFHyT4tCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNDDkZZl{KGK7IHPveYx1\XJiY3;1cpRmeiCvZYToc4QtKEmFNUC9NU46KM7:TR?= M4HXTFI{OTJ2MkGz
human SF539 cells NV7SSndJTnWwY4Tpc44h[XO|YYm= NFrXO3FKdmirYnn0bY9vKG:oIGDES2ZT[mW2YTDpckBpfW2jbjDTSlU{QSClZXzsd{BjgSCyaH;zdIhwfHm{b4PpcoUhTUyLU1GsJGlEPTB;Mj60JO69VQ>? MWOxPVc1QDd6NR?=
A431 cells MkTMSpVv[3Srb36gZZN{[Xl? NFzZRnpKdmirYnn0bY9vKG:oIG\FS2ZTOiCneIDy[ZN{\WRiaX6gbJVu[W5iQUSzNUBk\WyuczygTWM2OD1zMj65JO69VQ>? NFrBTY0zODV3OEC3Ni=>
HUVEC cells NUSzWId4WHKxbHnm[ZJifGmxbjDhd5NigQ>? MV63NkBp NF30b3pCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjVWmVEKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA4OiCqcoOgZpkhfHK7cHHuJIJtfWViYYPzZZktKEeLNUC9NVMvPiEQvF2= MkO5NlY{OThyNU[=
human HMEC1 cells NUPzbI1KWHKxbHnm[ZJifGmxbjDhd5NigQ>? MmrQO{Bl[Xm| NUTleVF3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIUWVEOSClZXzsd{Bi\nSncjC3JIRigXNiYomgZ492dHSncjDjc5VvfGW{IH3leIhw\CxiSVO1NF0yPSEQvF2= NFu3TWkzOzF{NEKxNy=>
human HeLa cells MnPlVJJwdGmoZYLheIlwdiCjc4PhfS=> NFSwZ4Q1KGSjeYO= NF3UfpNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IHPveYx1\XJiY3;1cpRmeiCvZYToc4QtKEmFNUC9NlAh|ryP MXeyN|EzPDJzMx?=

... Click to View More Cell Line Experimental Data

In vivo Semaxanib dose-related inhibits growth of A375 tumor in vivo. A >85% inhibition of subcutaneous tumor growth is observed with daily i.p. administration of SU5416 in DMSO at Semaxanib, without measurable toxicity. Semaxanib shows broad spectrum antitumor activity. SU5416 significantly inhibits the subcutaneous growth of 8 of 10 tumor lines tested (A431, Calu-6, C6, LNCAP, EPH4-VEGF, 3T3HER2, 488G2M2 and SF763T cells) with an average mortality rate of 2.5%. [1] Semaxanib (25 mg/kg/day) displays potent antiangiogenic activity, resulting in a significant reduction of both the total and functional vascular density of the tumor microvasculature. [2]


Kinase Assay:[1]
+ Expand

Biochemical kinase assays:

Solubilized membranes from 3T3 Flk-1 cells are added to polystyrene ELISA plates that had been precoated with a monoclonal antibody that recognizes Flk-1. After an overnight incubation with lysate at 4 ℃, serial dilutions of SU5416 are added to the immunolocalized receptor. To induce autophosphorylation of the receptor, various concentrations of ATP are added to the ELISA plate wells containing serially diluted solutions of SU5416. The autophosphorylation is allowed to proceed for 60 min at room temperature and then stopped with EDTA. The amount of phosphotyrosine present on the Flk-1 receptors in the individual wells is determined by incubating the immunolocalized receptor with a biotinylated monoclonal antibody directed against phosphotyrosine. After removal of the unbound anti-phosphotyrosine antibody, avidin-conjugated horseradish pero-idase H is added to the wells. A stabilized form of 3,3 9,5,5 9-tetramethyl benzidine dihydrochloride and H2O2 is added to the wells. The color readout of the assay is allowed to develop for 30 min, and the reaction is stopped with H2SO4.
Cell Research:[1]
+ Expand
  • Cell lines: HUVECs
  • Concentrations: ~100 μM
  • Incubation Time: 2 days
  • Method: HUVECs are plated in 96-well, flat-bottomed plates (1×104 cells/100 μL/well) in F-12K media containing 0.5% heat-inactivated FBS and cultured at 37 ℃ for 24 h to quiesce the cells. Serial dilutions of compounds prepared in medium containing 1% DMSO are then added for 2 h, followed by the addition of mitogenic concentrations of either VEGF at 5 ng/mL or 20 ng/mL or acidic fibroblast growth factor at 0.25–5 ng/mL in media. The final concentration of DMSO in the assay is 0.25%. After 24 h, either [3H]thymidine (1 μCi/well) or BrdUrd is added, and the cell monolayers are incubated for another 24 h. The uptake of either [3H]thymidine or BrdUrd into cells is quantitated using a liquid scintillation counter or a BrdUrd ELISA, respectively.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Human melanoma xenografts A375
  • Formulation: DMSO
  • Dosages: 25 mg/kg
  • Administration: i.p. daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 22 mg/mL (92.32 mM)
Ethanol 2 mg/mL (8.39 mM)
Water Insoluble
In vivo Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 238.28


CAS No. 194413-58-6
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00026377 Completed Prostate Cancer University of Chicago|National Cancer Institute (NCI) November 2001 Phase 1
NCT00023738 Completed Sarcoma Radiation Therapy Oncology Group|National Cancer Institute (NCI) August 2001 Phase 1|Phase 2
NCT00023725 Completed Sarcoma Radiation Therapy Oncology Group|National Cancer Institute (NCI) August 2001 Phase 1|Phase 2
NCT00017316 Completed Melanoma (Skin) National Cancer Institute (NCI) March 2001 Phase 2
NCT00009919 Terminated Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) December 2000 Phase 2
NCT00006361 Completed Carcinoma of Unknown Primary|Head and Neck Cancer|Non-melanomatous Skin Cancer Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) December 2000 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

VEGFR Signaling Pathway Map

Related VEGFR Products

Tags: buy Semaxanib (SU5416) | Semaxanib (SU5416) supplier | purchase Semaxanib (SU5416) | Semaxanib (SU5416) cost | Semaxanib (SU5416) manufacturer | order Semaxanib (SU5416) | Semaxanib (SU5416) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID