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.

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In DMSO USD 200 In stock
USD 170 In stock
USD 270 In stock
USD 970 In stock
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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

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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 M1XZdWN6fG:2b4jpZ4l1gSCjc4PhfS=> NUPIXnV4PDhiaB?= NEDQNnZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOS0Z5IHPlcIx{KGGodHXyJFQ5KGi{czDifUBES0t6IHHzd4F6NCCLQ{WwQVMvOSCwTR?= NXflW4N5OjN5N{e4PVg>
mouse B16F10 cells NUfsblZsS3m2b4TvfIlkcXS7IHHzd4F6 M{XuUVQ5KGh? MmjNR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRlE3TjFyIHPlcIx{KGGodHXyJFQ5KGi{czDifUBES0t6IHHzd4F6NCCLQ{WwQVMvPiCwTR?= M324[lI{Pzd5OEm4
human U251 cells MVfGeY5kfGmxbjDhd5NigQ>? M1;4cGlvcGmkaYTpc44hd2ZiVlXHSnIzKGmwIHj1cYFvKFV{NUGgZ4VtdHNiYomgdIhwe3Cqb4T5do9{cW6nIFXMTXNCNCCLQ{WwQVEzNjlibl2= NV7BcFQ2OjR7MEC4OlU>
human A431 cells NFrrdI1HfW6ldHnvckBie3OjeR?= MnzjRY51cWGwZ3nv[4VvcWNiYXP0bZZqfHliYXfhbY5{fCCqdX3hckBCPDNzIHPlcIx{NCCLQ{WwQVAvODh3IN88US=> NHe1[nMzODRyM{[5Ny=>
CHO cells NF35[G9HfW6ldHnvckBie3OjeR?= MX3Jcohq[mm2aX;uJI9nKF[HR1\SJIlv\HWlZXSgZZV1d3Cqb4PwbI9zgWyjdHnvckBw\iCqdX3hckBX[XOldXzhdkBmdmSxdHjlcIlidCCpcn;3eIgh\mGldH;yJJJm[2WydH;yJFIhMF[HR1\SNkkhfHKjboPm[YN1\WRiaX6gR2hQKGOnbHzzMEBKSzVyPUCuPFg1KM7:TR?= MVSxNlQ4PzN3Mh?=
human MCF7 cells NX;XRlBnWHKxbHnm[ZJifGmxbjDhd5NigQ>? MX:0JIRigXN? MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPCCmYYnzJIJ6KGOxdXz0[ZIh[2:3boTldkBu\XSqb3SsJGlEPTB;MT65JO69VQ>? MlnzNlMyOjR{MUO=
human SF539 cells NWraRXBnTnWwY4Tpc44h[XO|YYm= M1LRWmlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHnuJIh2dWGwIGPGOVM6KGOnbHzzJIJ6KHCqb4PwbI91gXKxc3nu[UBGVEmVQTygTWM2OD1{LkSg{txO MlLRNVk4PDh5OEW=
A431 cells NHSySnZHfW6ldHnvckBie3OjeR?= M4jMR2lvcGmkaYTpc44hd2ZiVlXHSnIzKGW6cILld5Nm\CCrbjDoeY1idiCDNEOxJINmdGy|LDDJR|UxRTF{Lkmg{txO MknyNlA2PThyN{K=
HUVEC cells NFnzfplRem:uaX\ldoF1cW:wIHHzd4F6 NXv4Zpp4PzJiaB?= MVTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiXVlXDJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgeJJ6eGGwIHLseYUh[XO|YYmsJGdKPTB;MUOuOkDPxE1? MWGyOlMyQDB3Nh?=
human HMEC1 cells NEXsdJdRem:uaX\ldoF1cW:wIHHzd4F6 NX:xdm9LPyCmYYnz MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiPRVOxJINmdGy|IHHmeIVzKDdiZHH5d{BjgSClb4XseIVzKGOxdX70[ZIhdWW2aH;kMEBKSzVyPUG1JO69VQ>? NGfMU4wzOzF{NEKxNy=>
human HeLa cells MojvVJJwdGmoZYLheIlwdiCjc4PhfS=> NU\SNnVWPCCmYYnz NEfRbJBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjlUIEh[2WubIOgZYZ1\XJiNDDkZZl{KGK7IHPveYx1\XJiY3;1cpRmeiCvZYToc4QtKEmFNUC9NlAh|ryP MkX1NlMyOjR{MUO=

... 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 to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
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
in solvent
Synonyms N/A

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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
NCT00021281 Unknown status Colorectal Cancer Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI) December 2000 Phase 3
NCT00009919 Terminated Recurrent Renal Cell Cancer|Stage IV Renal Cell Cancer National Cancer Institute (NCI) December 2000 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID