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CAS No. 194413-58-6; 204005-46-9
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.
Selleck's Semaxanib (SU5416) has been cited by 12 publications
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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.
HUVEC spheroids embedded in fibrin gel were incubated with a pool of PDR vitreous fluid samples (1:4 dilution) in the absence or in the presence of different extracellular pathway. Formation of radially growing sprouts was evaluated after 24 h of incubation. Data are the mean ± S.E.M. of 30 spheroids per experimental point. *p《0.05, **p《0.01 versus PDR vitreous
Angiogenesis, 2017, 20(4):629-640. Semaxanib (SU5416) purchased from Selleck.
VEGFR inhibition mitigates JNA fibroblast-induced tubule formation in HUVECS. (A) HUVEC tubule formation was assessed in the presence of JNA CM or SFM with or without SU5416 or vehicle control (DMSO). The photograph represents characteristic HUVEC tubules in each treatment group. (B) HUVECs were plated on a layer of Matrigel in the presence of SFM or JNA CM and subsequently treated with vehicle control (DMSO) or SU5416 at an IC50 concentration of 1.23µM. After a 6-hour incubation at 37°C, the HUVECs were examined under magnification ×100 and tubule formation and length were assessed using Pipeline software. The experiment was repeated 3 times. CM = conditioned media; DMSO = dimethylsulfoxide; HUVEC = human umbilical vein endothelial cell; IC50 = the dose that is cytotoxic to 50% of the cells treated in vitro; JNA = juvenile nasopharyngeal angiofibroma; SFM = serum-free media.
Int Forum Allergy Rhinol, 2017, 7(10):973-979. Semaxanib (SU5416) purchased from Selleck.
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Choose Selective VEGFR Inhibitors
|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.|
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). 
|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%.  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. |
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.
|In vitro||DMSO||22 mg/mL (92.32 mM)|
|Ethanol||2 mg/mL (8.39 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40%PEG 300+ 5% Tween80 + ddH2O
For best results, use promptly after mixing.
* 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.
|CAS No.||194413-58-6; 204005-46-9|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT00006247||Terminated||Drug: semaxanib||Brain and Central Nervous System Tumors||Pediatric Brain Tumor Consortium|National Cancer Institute (NCI)||August 2000||Phase 1|
|NCT00005642||Completed||Drug: semaxanib||Unspecified Adult Solid Tumor Protocol Specific||Case Comprehensive Cancer Center|National Cancer Institute (NCI)||May 2000||Phase 1|
|NCT00005647||Completed||Drug: paclitaxel|Drug: semaxanib||Head and Neck Cancer||Case Comprehensive Cancer Center|National Cancer Institute (NCI)||May 2000||Phase 1|
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