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NVP-ACC789  ≥98%

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包装规格：5mg 10mg 25mg 50mg in glass bottle
溶解性：溶于DMSO（25mg/mL超声）
产品描述：基本信息 产品编号：N11191 产品名称：NVP-ACC789 CAS: 300842-64-2   储存条件 粉末 -20℃ 四年     分子式： C21H17BrN4 溶于液体 -80℃ 六个月 分子量 405.30 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO   Ethanol   Water   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 2.4674mL 12.3368mL 24.6737mL 5mM 0.4935mL 2.4674mL 4.9347mL 10mM 0.2467mL 1.2337mL 2.4674mL   生物活性 产品描述 一种人 VEGFR-1，VEGFR-2 (鼠 VEGFR-2)，VEGFR-3 和 PDGFR-β 的抑制剂，IC50 值分别为 0.38，0.02 (0.23)，0.18 和 1.4μM。 靶点/IC50 VEGFR-2 0.02μM (IC50) VEGFR-1 0.38μM (IC50) mVEGFR-2 0.23μM (IC50) VEGFR-3 0.18μM (IC50) PDGFR-β 1.4μM (IC50)         体外研究 The enzymatic kinase assays demonstrate that NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4μM,respectively. In VEGF-treated cultures, addition of the VEGFR-2 inhibitor NVP-ACC789 reduces BME cell number to baseline levels from 1μM. Likewise, bFGF-induced BME cell proliferation is reduced markedly by NVP-ACC789 from 1 to 10μM, without however reaching basal levels. NVP-ACC789 is found to be a potent inhibitor of VEGF-induced HUVE cell proliferation with an IC50 of 1.6nM. NVP-ACC789 also completely inhibits VEGF-induced BME and BAE cell invasion and VEGF-C-induced BAE cell invasion. The inhibition is dose-dependent in both cell types with a maximal effect from 1μM. 体内研究 NVP-ACC789 which is given in daily oral doses for 6 days blocks VEGF-induced angiogenesis in a dose-dependent manner. NVP-ACC789 also inhibits the response to bFGF to some extent, but the dose-response curve is not linear for NVP-ACC789.   推荐实验方法(仅供参考) 激酶实验： Human VEGFR-2-transfected CHO cells are seeded into 6-well plates and grown to about 80% confluency. NVP-ACC789 is added in serial dilutions and the cells incubated for 2h at 37°C in medium without fetal calf serum (FCS). VEGF (20ng/mL) is then added. After a 5-min incubation at 37°C, the cells are washed twice with ice-cold phosphate-buffered saline and lysed. Nuclei are removed by centrifugation for 10 min at 4°C. Protein concentrations of the lysates are determined.   细胞实验:   HUVE cell proliferation is determined. Cells are seeded into 1.5% gelatin-coated 96-well plates (5×103 cells per well) and incubated in endothelial cell growth medium containing 5% fetal calf serum (FCS) for 24h. The medium is replaced with essential basic medium (1.5% FCS), and the cells are incubated for another 24 h. Essential basic medium is then replaced with fresh medium containing either 50ng/mL VEGF or 0.5ng/mL bFGF. NVP-ACC789 is added just before addition of growth factors. The cells are incubated for a further 24h before adding the BrdU labeling solution. Twenty four hours later, the labeling solution is removed, the cells are fixed, and the incorporated BrdU is visualized with a peroxidase-labeled anti-BrdU antibody and TMB substrate.   动物实验:   Porous Teflon chambers (volume, 0.5mL) filled with 0.8% w/v agar-containing heparin (20U/mL) with or without VEGF (2μg/mL) or bFGF (0.3μg/mL) are implanted subcutaneously on the dorsal flank of female mice. The mice are treated with NVPACC789 (p.o. once daily) or vehicle (5% dimethyl sulfoxide,1% Tween 80 in water) starting 1 day before implantation of the chamber and continuing for 5 days thereafter.At the end of the treatment period, the mice are killed,and the chambers are removed.The vascularized tissue growing around the chamber is removed carefully and weighed,and the blood content is assessed by measuring hemoglobin levels.The percentage inhibition of the angiogenic response (increase in tissue weight or total blood) is calculated.EC50 values are estimated from the dose response curves (% inhibition versus dose).Each experiment is performed with six animals per dose group and each dose is tested in at least two independent experiments.
保存条件：-20℃

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