SU1498  ≥98%

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熔点:126 °C
包装规格:1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
产品简介:SU1498 (AG 1498) 是选择性的 VEGFR2 抑制剂;抑制 Flk-1 的 IC50 值为 700 nM。
溶解性:DMSO :78 mg/mL (199.73 mM) Ethanol:78 mg/mL (199.73 mM) Water:Insoluble
储备液保存:-80°C 2 years -20°C 1 year
体内实验:1、请依序添加每种溶剂: 10% DMSO→40% PEG300 →5% Tween-80 →45% saline Solubility: ≥ 2.5 mg/mL (6.40 mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (6.40 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2、请依序添加每种溶剂: 10% DMSO→90% (20% SBE-β-CD in saline) Solubility: 2.5 mg/mL (6.40 mM); Suspended solution; Need ultrasonic 此方案可获得 2.5 mg/mL (6.40 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 <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。
靶点:Flk-1:700 nM (IC50)
体外研究:SU1498 stimulates accumulation of phosphorylated ERKs in human umbilical vein endothelial cells and in human aortic endothelial cells in a manner that is dependent on the functioning of the upstream components of the MAPK pathway, B-Raf, and MEK kinases. The enhanced accumulation of phospho-ERKs is observed only in cells that have been stimulated with sphingosine 1-phosphate or protein growth factors; SU1498 by itself is ineffective. SU1498 blocks signal transduction from VEGFR2 in MS1 VEGF cells.In the presence of SU1498, levels of Ets-1 are decreased, suggesting that VEGF-VEGFR-2 interactions contributed to baseline levels of Ets-1 expression, and interruption of this autocrine interaction with SU1498 led to decreased expression of Ets-1. SU1498 treatment significantly impacts U87 cell proliferation and apoptosis. SU1498 induces a marked increase in lipids and a decrease in glycerophosphocholine. Accordingly, accumulation of lipid droplets is seen in the cytoplasm of SU1498-treated U87 cells.
保存条件:-20°C
注意事项:1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。