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Semaxanib (SU5416)

Name: Semaxanib (SU5416)
Brand: Selleck Chemicals
SKU: S2845
Rating: 5 (16 reviews)

Catalog No.S2845 Synonyms: semaxinib

For research use only.

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.

CAS No. 194413-58-6, 204005-46-9

Selleck's Semaxanib (SU5416) has been cited by 16 publications

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VEGFR Signaling Pathway Map

Biological Activity

Description

Targets

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	NG[5PYdEgXSxdH;4bYNqfHliYYPzZZk>	MnvXOFghcA>?	Mn7PR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC0PEBpenNiYomgR2NMQCCjc4PhfUwhUUN3ME2zMlEhdk1?	NUfNU4g5OjN5N{e4PVg>
mouse B16F10 cells	M4nXdGN6fG:2b4jpZ4l1gSCjc4PhfS=>	MWq0PEBp	M4TZU2N6fG:2b4jpZ4l1gSCjZ3HpcpN1KG2xdYPlJGIyPkZzMDDj[YxteyCjZoTldkA1QCCqcoOgZpkhS0ONODDhd5NigSxiSVO1NF0{NjZibl2=	Mn\kNlM4Pzd6OUi=
human U251 cells	MlXmSpVv[3Srb36gZZN{[Xl?		MVHJcohq[mm2aX;uJI9nKF[HR1\SNkBqdiCqdX3hckBWOjVzIHPlcIx{KGK7IIDoc5NxcG:2eYLvd4lv\SCHTFnTRUwhUUN3ME2xNk46KG6P	NX3TZ5dpOjR7MEC4OlU>
human A431 cells	NHTydJRHfW6ldHnvckBie3OjeR?=		MXfBcpRq[W6paX;n[Y5q[yCjY4Tpeol1gSCjZ3HpcpN1KGi3bXHuJGE1OzFiY3XscJMtKEmFNUC9NE4xQDVizszN	MnTPNlA1ODN4OUO=
CHO cells	NU[zVHZtTnWwY4Tpc44h[XO\|YYm=		M3i0PGlvcGmkaYTpc44hd2ZiVlXHSnIhcW6mdXPl[EBifXSxcHjvd5Bpd3K7bHH0bY9vKG:oIHj1cYFvKF[jc3P1cIFzKGWwZH;0bIVtcWGuIHfyc5d1cCCoYXP0c5IhemWlZYD0c5IhOiBqVlXHSnIzMSC2cnHud4Zm[3SnZDDpckBEUE9iY3XscJMtKEmFNUC9NE45QDRizszN	NXLOcolROTJ2N{ezOVI>
human MCF7 cells	NHTIRlZRem:uaX\ldoF1cW:wIHHzd4F6	Mkn4OEBl[Xm\|	M{KwcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB2IHThfZMh[nliY3;1cJRmeiClb4XueIVzKG2ndHjv[EwhUUN3ME2xMlkh\|ryP	NFnqTYwzOzF{NEKxNy=>
human SF539 cells	NEL1SZlHfW6ldHnvckBie3OjeR?=		M4XMdmlvcGmkaYTpc44hd2ZiUFTHSnJj\XSjIHnuJIh2dWGwIGPGOVM6KGOnbHzzJIJ6KHCqb4PwbI91gXKxc3nu[UBGVEmVQTygTWM2OD1{LkSg{txO	NE\hWG8yQTd2OEe4OS=>
A431 cells	NGLXUI5HfW6ldHnvckBie3OjeR?=		MWLJcohq[mm2aX;uJI9nKF[HR1\SNkBmgHC{ZYPz[YQhcW5iaIXtZY4hSTR\|MTDj[YxteyxiSVO1NF0yOi57IN88US=>	MkKxNlA2PThyN{K=
HUVEC cells	NFm0WlVRem:uaX\ldoF1cW:wIHHzd4F6	M2H2WlczKGh?	MljrRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKVW\FR{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3XscEB3cWGkaXzpeJkh[W[2ZYKgO\|IhcHK\|IHL5JJRzgXCjbjDicJVmKGG\|c3H5MEBIUTVyPUGzMlYh\|ryP	MoSxNlY{OThyNU[=
human HMEC1 cells	M{jXNnBzd2yrZnXyZZRqd25iYYPzZZk>	NH3qNHI4KGSjeYO=	NEHmVmdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjNSWMyKGOnbHzzJIFnfGW{IEeg[IF6eyCkeTDjc5VtfGW{IHPveY51\XJibXX0bI9lNCCLQ{WwQVE2KM7:TR?=	NHnL[pozOzF{NEKxNy=>
human HeLa cells	NULkPWF1WHKxbHnm[ZJifGmxbjDhd5NigQ>?	NF7RXmM1KGSjeYO=	MoDqRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKZVzhJINmdGy\|IHHmeIVzKDRiZHH5d{BjgSClb4XseIVzKGOxdX70[ZIhdWW2aH;kMEBKSzVyPUKwJO69VQ>?	NFvoZYczOzF{NEKxNy=>

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

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

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]

Protocol (from reference)

Kinase Assay:^[1]	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]	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.
Animal Research:^[1]	Animal Models: Human melanoma xenografts A375 Dosages: 25 mg/kg Administration: i.p. daily

References

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): 5% DMSO+40%PEG 300+ 5% Tween80 + ddH2O For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	0.5mg/mlmg/mL

Chemical Information

Molecular Weight	238.28
Formula	C₁₅H₁₄N₂O
CAS No.	194413-58-6, 204005-46-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=CC(=C(N1)C=C2C3=CC=CC=C3NC2=O)C

Download Semaxanib (SU5416) SDF

In vivo Formulation Calculator (Clear solution)

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

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

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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
NCT00005647	Completed	Drug: paclitaxel\|Drug: semaxanib	Head and Neck Cancer	Case Comprehensive Cancer Center\|National Cancer Institute (NCI)	May 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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