(Z)-Semaxinib
作者：齊岳
發(fā)布時間：2023-08-29
13:38:47
點擊數(shù)：
產(chǎn)品名稱：(Z)-Semaxinib
產(chǎn)品描述：
| 產(chǎn)品描述 | 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. |
| 靶點活性 | VEGFR2/Flk1:1.23 μM |
| 體外活性 | 在10種測試細胞系中,Semaxanib對其中8種(A431,Calu-6,C6,LNCAP,EPH4-VEGF,3T3HER2,488 g2M2以及SF763T細胞)的皮下生長均有明顯抑制作用,平均死亡率為2.5%.Semaxanib劑量依賴性抑制體內(nèi)A375的生長.Semaxanib（25 mg/kg/day）具有較強抗血管生成活性,顯著降低微血管系統(tǒng)的總功能性血管密度.Semaxanib（i.p.）可抑制>85%的皮下生長,且無可檢測的毒性. |
| 體內(nèi)活性 | Semaxanib劑量依賴性抑制VEGF（IC50：0.04 μM）和FGF（IC50：50 μM）誘導(dǎo)的有絲分裂。Semaxanib不影響C6膠質(zhì)瘤,Calu 6肺*,A375黑素瘤,A431 鱗狀細胞*,和SF767T 神經(jīng)膠質(zhì)瘤細胞在體外的生長（IC50s>20 μM）。在Flk-1過表達的NIH 3T3細胞中,Semaxanib對Flk-1受體的VEGF-依賴性磷酸化具有抑制作用（IC50：1.04 μM）。Semaxanib可抑制NIH 3T3細胞中PDGF依賴性自身磷酸化（IC50：20.3 μM）。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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.(Only for Reference) |
| 別名 | SU5416 |
| 分子量 | 238.28 |
| 分子式 | C15H14N2O |
| CAS No. | 194413-58-6 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
DMSO: 21 mg/mL (88.1 mM)
Ethanol: 2 mg/mL (8.39 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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