Semaxanib (SU5416)

製品コードS2845 バッチS284503

印刷

化学情報

Chemical Structure Synonyms semaxinib Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C15H14N2O
分子量 238.28 CAS No. 204005-46-9
Solubility (25°C)* 体外 DMF 100 mg/mL (419.67 mM)
DMSO 20 mg/mL (83.93 mM)
Ethanol 4 mg/mL (16.78 mM)
体内 （毎回新しく調製した物を用意してください）
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 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 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 40% PEG 300 5%Tween80 45%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 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. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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) can be used to induce animal models of Chronic Intermittent Hypoxia.
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 it also inhibits PDGF-dependent autophosphorylation in NIH 3T3 cells with IC50 of 20.3 μM. This compound inhibits VEGF- and FGF-driven mitogenesis in a dose-dependent manner with IC50 of 0.04 and 50 μM, respectively. Its 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]
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]

プロトコル(参考用のみ)

キナーゼアッセイ 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 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.
細胞アッセイ 細胞株 HUVECs
濃度 ~100 μM
反応時間 2 days
実験の流れ 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 Semaxanib (SU5416) 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.
動物実験 動物モデル Human melanoma xenografts A375
投薬量 25 mg/kg
投与方法 i.p. daily

参考

  • https://pubmed.ncbi.nlm.nih.gov/9892193/
  • https://pubmed.ncbi.nlm.nih.gov/10935468/

カスタマーフィードバック

Data from [Data independently produced by , , Sci Rep, 2016, 6:19304. ]

Data from [Data independently produced by , , Angiogenesis, 2017, 20(4):629-640]

Data from [Data independently produced by , , Int Forum Allergy Rhinol, 2017, 7(10):973-979]

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VEGF Modulates Neurogenesis and Microvascular Remodeling in Epileptogenesis After Status Epilepticus in Immature Rats [ Front Neurol, 2021, 12:808568] PubMed: 35002944
PKR deficiency alleviates pulmonary hypertension via inducing inflammasome adaptor ASC inactivation [ Pulm Circ, 2021, 11(4):20458940211046156] PubMed: 34540200

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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