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Angiogenesis VEGFR (Z)-Semaxinib

(Z)-Semaxinib

Catalog No. T2496   CAS 194413-58-6
Synonyms: Semaxanib, SU5416,
Purity 100.00% Datasheet MSDS

Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR over PDGFRβ, no inhibition for FGFR, InsR, and EGFR. Semaxanib is a quinolone derivative with potential antineoplastic activity.

(Z)-Semaxinib, CAS 194413-58-6
Pack Size Availability Price/USD Quantity
1 mg In stock 58.00
2 mg In stock 70.00
5 mg In stock 127.00
10 mg In stock 224.00
25 mg In stock 388.00
50 mg In stock 670.00
1 mL * 10 mM (in DMSO) In stock 164.00
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Purity 96.09%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR over PDGFRβ, no inhibition for FGFR, InsR, and EGFR. Semaxanib is a quinolone derivative with potential antineoplastic activity.
Targets&IC50 VEGFR2/Flk1 :ic50 1.23μM,  
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 Water2 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
HUVECs are plated in 96-well, flat-bottomed plates (1&times104 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.(Only for Reference)
Cell lines: HUVECs
Animal Research
Animal Model: Human melanoma xenografts A375
Synonyms Semaxanib, SU5416,
Purity 99.94%
Appearance solid
Molecular Weight 238.28
Formula C15H14N2O
CAS No. 194413-58-6

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 21 mg/mL (88.1 mM)

Ethanol: 2 mg/mL (8.39 mM)

Water: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL

Citations

References and Literature
1. Fong TA, et al. Cancer Res, 1999, 59(1), 99-106. 2. Vajkoczy P, et al. Neoplasia, 1999, 1(1), 31-41.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Tyrosine kinase inhibitor library Cytokine Inhibitor Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Angiogenesis related Compound Library

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