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Semaxanib (SU5416)

Name: Semaxanib (SU5416)
Brand: Selleck Chemicals
SKU: S2845
Rating: 5 (19 reviews)

Synonyms: semaxinib

Catalog No.S2845 Purity:99.99%

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

CAS No. 204005-46-9

Purity & Quality Control

Batch: Purity: 99.99%

99.99

Semaxanib (SU5416) Related Products

Related Targets	VEGFR1 VEGFR2 VEGFR3	Click to Expand
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Related Compound Libraries	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	Click to Expand

Signaling Pathway

VEGFR Signaling Pathway

Cell Data

Cell Lines	Assay Type	Incubation Time	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
Click to View More Cell Line Experimental Data

Biological Activity

Description

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
Kinase Assay	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

References

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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.					In vivo Formulation Calculator
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.28mg/ml (1.18mM)	Taking the 1 mL working solution as an example, add 50 μL 5.6 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to make it clear. Volume up to 1 mL. The mixed solution should be used immediately for optimal results.	In vivo Formulation Calculator
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.4mg/ml (1.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% corn oil	0.8mg/ml (3.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 16 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.5mg/ml (2.10mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	10% DMF 1 40% PEG 300 2 5%Tween80 3 45%ddH2O	3.3mg/ml (13.85mM)	Taking the 1 mL working solution as an example, add 100μL of 33mg/ml clarified DMF stock solution to 400μL of PEG300, mix evenly to clarify it; add 50μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 450μL of ddH2O to adjust the volume to 1mL. The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

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