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Semaxanib (SU5416) VEGFR2 inhibitor

Name: Semaxanib (SU5416)
SKU: S2845
Availability: InStock
Rating: 5 (21 reviews)

Cat.No.S2845

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, and lacks activity against EGFR, InsR and FGFR. Phase 3. It can be used to induce animal models of chronic intermittent hypoxia.

Chemical Structure

Molecular Weight: 238.28

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	EGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
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Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
MCF7 cells	Cytotoxicity assay	48 h	Cytotoxicity against human MCF7 cells after 48 hrs by CCK8 assay, IC50=3.1 nM
mouse B16F10 cells	Cytotoxicity assay	48 h	Cytotoxicity against mouse B16F10 cells after 48 hrs by CCK8 assay, IC50=3.6 nM
human U251 cells	Function assay		Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA, IC50=12.9 nM
human A431 cells	Function assay		Antiangiogenic activity against human A431 cells, IC50=0.085 μM
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
human MCF7 cells	Proliferation assay	4 days	Antiproliferative activity against human MCF7 cells after 4 days by coulter counter method, IC50=1.9 μM
human SF539 cells	Function assay		Inhibition of PDGFRbeta in human SF539 cells by phosphotyrosine ELISA, IC50=2.4 μM
A431 cells	Function assay		Inhibition of VEGFR2 expressed in human A431 cells, IC50=12.9 μM
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
human HMEC1 cells	Proliferation assay	7 days	Antiproliferative activity against human HMEC1 cells after 7 days by coulter counter method, IC50=15 μM
human HeLa cells	Proliferation assay	4 days	Antiproliferative activity against human HeLa cells after 4 days by coulter counter method, IC50=20 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight	238.28	Formula	C₁₅H₁₄N₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	204005-46-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	semaxinib			Smiles	CC1=CC(=C(N1)C=C2C3=CC=CC=C3NC2=O)C

Solubility

In vitro
Batch:

DMSO : 17 mg/mL (71.34 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

DMSO : 40 mg/mL (167.86 mM) Warmed with 50°C water bath; Ultrasonicated;
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.280mg/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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.800mg/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.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.300mg/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.

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.

Mechanism of Action

Targets/IC₅₀/Ki	VEGFR2/Flk1 ^[1] (Cell-free assay) 1.23 μM
In vitro	Semaxanib (SU5416) inhibits VEGF-dependent phosphorylation of the Flk-1 receptor in Flk-1-overexpressing NIH 3T3 cells with IC50 of 1.04 μM, and PDGF-dependent autophosphorylation in NIH 3T3 cells with IC50 of 20.3 μM. It also inhibits VEGF- and FGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 and 50 μM, respectively. Treatment with this compound 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 Semaxanib (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 this compound. 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 vivo	Semaxanib (SU5416) dose-related inhibits growth of A375 tumor in vivo. A >85% inhibition of subcutaneous tumor growth is observed with daily i.p. administration of this compound in DMSO, without measurable toxicity. It shows broad spectrum antitumor activity, significantly inhibiting 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] At 25 mg/kg/day, it displays potent antiangiogenic activity, resulting in a significant reduction of both the total and functional vascular density of the tumor microvasculature. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/9892193/ [2] https://pubmed.ncbi.nlm.nih.gov/10935468/

Applications

Methods	Biomarkers	Images	PMID
Western blot	p-VEGFR2 / VEGFR2 / p-PLCγ1 / PLCγ1 / p-ERK / ERK		21699503
Immunofluorescence	CD31 / OCT-4 / SOX-2		25665868

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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