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SU14813  ≥98%

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溶解性：溶于DMSO（40mg/mL超声）
产品描述：基本信息 产品编号：S11098 产品名称：SU14813 CAS: 627908-92-3   储存条件 粉末 -20℃ 四年     分子式： C23H27FN4O4 溶于液体 -80℃ 六个月 分子量 442.48 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 88mg/mL (198.87mM) Ethanol Insoluble Water Insoluble 体内（现配现用）     ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.2600mL 11.2999mL 22.5999mL 5mM 0.4520mL 2.2600mL 4.5200mL 10mM 0.2260mL 1.1300mL 2.2600mL 50mM 0.0452mL 0.2260mL 0.4520mL   生物活性 产品描述 是多靶点受体酪氨酸激酶抑制剂，抑制 VEGFR2，VEGFR1，PDGFRβ and KIT 的 IC50 值分别为50，2，4，15nM。 靶点/IC50 VEGFR1(Cell-free assay) PDGFRβ(Cell-free assay) KIT(Cell-free assay) VEGFR2(Cell-free assay) 2nM 4nM 15nM 50nM   体外研究 SU14813 inhibits ligand-dependent and ligand-independent proliferation, migration, and survival of endothelial cells and/or.tumor cells expressing these targets. SU14813 inhibits cellular ligand-dependent phosphorylation of VEGFR-2 (transfected NIH 3T3 cells), PDGFR-β (transfected NIH 3T3 cells), KIT (Mo7e cells), and FLT3-internal tandem duplication (FLT3-ITD;MV4;11 cells) as well as FMS/CSF1R (transfected NIH 3T3 cells). SU14813 inhibits VEGFR-2, PDGFR-β, and KIT phosphorylation in porcine aorta endothelial cells overexpressing these targets, with cellular IC50 values of 5.2, 9.9, and 11.2nM,respectively.SU14813 inhibits the growth of U-118MG with an IC50 of 50 to 100nM.   体内研究 SU14813 inU14813 inhibits VEGFR-2, PDGFR-β, and FLT3 phosphorylation in xenograft tumors in a dose- and time-dependent fashion.The plasma concentration required for in vivo target inhibition is estimated to be 100 to 200ng/mL. Used as monotherapy,SU14813 exhibits broad and potent antitumor activity resulting in regression, growth arrest, or substantially reduces growth of various established xenografts derived from human or rat tumor cell lines. Treatment in combination with docetaxel significantly enhances both the inhibition of primary tumor growth and the survival of the tumor-bearing mice compared with administration of either agent alone.   推荐实验方法(仅供参考) 细胞实验:   The effect of SU14813 on endothelial cell survival is evaluated. Passages 4 to 5 human umbilical vein endothelial cells are grown to subconfluency in EGM2 medium containing 10% FBS,endothelial cell growth supplement, and 10μg/mL sodium heparin. The cells are seeded in 96-well plates at 10,000 per well in F12K medium and 10% FBS. The next day, cells are starved for 18 hours in F12K+1% FBS and then incubated with SU14813 in various concentrations. 45 minutes later, 20ng/mL growth factor [VEGF or basic fibroblast growth factor (bFGF)] is introduced into the assay. Three days later, cell numbers are determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay.   动物实验:   Mouse: SU14813 is evaluated for its efficacy and synergism in combination with the microtubule inhibitor docetaxel in docetaxel-resistant murine LLC model. SU14813 is administered p.o. twice daily (BID) at doses of 10, 40, 80, or 120mg/kg beginning on day 5 after tumor implantation. Docetaxel 40mg/kg (mouse maximum tolerated dose) is administered i.v.thrice weekly also beginning on day 5 after tumor implantation.
保存条件：-20℃

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