Semaxanib (SU5416)

Synonyms: semaxinib

Semaxanib (SU5416, semaxinib) 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 (SU5416) Chemical Structure

Semaxanib (SU5416) Chemical Structure

CAS: 204005-46-9

Selleck's Semaxanib (SU5416) has been cited by 17 Publications

3 Customer Reviews

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Semaxanib (SU5416) Related Products

Signaling Pathway

Choose Selective VEGFR Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells after 48 hrs by CCK8 assay, IC50=3.1 nM 23777898
mouse B16F10 cells Cytotoxicity assay 48 h Cytotoxicity against mouse B16F10 cells after 48 hrs by CCK8 assay, IC50=3.6 nM 23777898
human U251 cells Function assay Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50=12.9 nM 24900865
human A431 cells Function assay Antiangiogenic activity against human A431 cells, IC50=0.085 μM 20403693
CHO cells Function assay Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells, IC50=0.884 μM 12477352
human MCF7 cells Proliferation assay 4 days Antiproliferative activity against human MCF7 cells after 4 days by coulter counter method, IC50=1.9 μM 23124213
human SF539 cells Function assay Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine ELISA, IC50=2.4 μM 19748785
A431 cells Function assay Inhibition of VEGFR2 expressed in human A431 cells, IC50=12.9 μM 20558072
HUVEC cells Proliferation assay 72 h Antiproliferative activity against human HUVEC cells assessed as reduction in cell viability after 72 hrs by trypan blue assay, GI50=13.6 μM 26318056
human HMEC1 cells Proliferation assay 7 days Antiproliferative activity against human HMEC1 cells after 7 days by coulter counter method, IC50=15 μM 23124213
human HeLa cells Proliferation assay 4 days Antiproliferative activity against human HeLa cells after 4 days by coulter counter method, IC50=20 μM 23124213
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Biological Activity

Description Semaxanib (SU5416, semaxinib) 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.
Targets
VEGFR2/Flk1 [1]
(Cell-free assay)
1.23 μM
In vitro
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]
Kinase Assay 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 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-VEGFR2 / VEGFR2 / p-PLCγ1 / PLCγ1 / p-ERK / ERK 21699503
Immunofluorescence CD31 / OCT-4 / SOX-2 25665868
In Vivo
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]
Animal Research Animal Models Human melanoma xenografts A375
Dosages 25 mg/kg
Administration i.p. daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00006247 Terminated
Brain and Central Nervous System Tumors
Pediatric Brain Tumor Consortium|National Cancer Institute (NCI)
August 2000 Phase 1
NCT00005642 Completed
Unspecified Adult Solid Tumor Protocol Specific
Case Comprehensive Cancer Center|National Cancer Institute (NCI)
May 2000 Phase 1
NCT00005647 Completed
Head and Neck Cancer
Case Comprehensive Cancer Center|National Cancer Institute (NCI)
May 2000 Phase 1

Chemical Information & Solubility

Molecular Weight 238.28 Formula

C15H14N2O

CAS No. 204005-46-9 SDF Download Semaxanib (SU5416) SDF
Smiles CC1=CC(=C(N1)C=C2C3=CC=CC=C3NC2=O)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 17 mg/mL ( (71.34 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble


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In vivo
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