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N-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide  100%

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包装规格：10mg 50mg 250mg in glass bottle
溶解性：溶于DMSO（≥100mg/mL）
产品描述：基本信息 产品编号：M11524 产品名称：N-(3,3-dimethylindolin-6-yl)-2-(pyridin-4-ylmethylamino)nicotinamide CAS: 453562-69-1   储存条件 粉末 -20℃ 四年     分子式： C22H23N5O 溶于液体 -80℃ 六个月 分子量 373.46 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 18.2mg/mL (48.73mM) Ethanol 8mg/mL (21.42mM) 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 2.6777mL 13.3887mL 26.7773mL 5mM 0.5355mL 2.6777mL 5.3555mL 10mM 0.2678mL 1.3389mL 2.6777mL   生物活性 产品描述 一种有效的 VEGFR1/2/3 的 ATP 竞争性抑制剂，IC50 值2nM/3nM/6 nM，与对 Kit 的选择性相似，是 PDGFR 和 Ret 的 10 倍多。 靶点/IC50 VEGFR1 2nM (IC50) VEGFR2 3nM (IC50) VEGFR3 6nM (IC50)   体外研究 Motesanib has broad activity against the human VEGFR family, and displays > 1000 selectivity against EGFR, Src, and p38 kinase. Motesanib significantly inhibits VEGF-induced cellular proliferation of HUVECs with an IC50 of 10nM, while displaying little effect at bFGF-induced proliferation with an IC50 of >3,000nM. Motesanib also potently inhibits PDGF-induced proliferation and SCF-induced c-kit phosphorylation with IC50 of 207nM and 37nM, respectively, but not effective against the EGF-induced EGFR phosphorylation and cell viability of A431 cells[1]. Althouth displaying little antiproliferative activity on cell growth of HUVECs alone, Motesanib treatment significantly sensitizes the cells to fractionated radiation.   体内研究 Motesanib (100mg/kg) significantly inhibits VEGF-induced vascular permeability in a time-dependent manner. Oral administration of Motesanib twice daily or once daily potently inhibits, in a dose-dependent manner, VEGF-induced angiogenesis using the rat corneal model with ED50 of 2.1mg/kg and 4.9mg/kg, respectively. Motesanib induces a dosedependent tumor regression of established A431 xenografts by selectively targeting neovascularization in tumor cells.Motesanib in combination with radiation displays significant anti-tumor activity in head and neck squamous cell carcinoma.(HNSCC) xenograft models. Motesanib treatment also induces significant dose-dependent reductions in tumor growth and blood vessel density of MCF-7, MDA-MB-231, or Cal-51 xenografts, which can be markedly enhanced when combined with docetaxel or tamoxifen.   推荐实验方法(仅供参考) 激酶实验： Optimal enzyme, ATP, and substrate (gastrin peptide) concentrations are established for each enzyme using homogeneous time-resolved fluorescence (HTRF) assays. Motesanib is tested in a 10-point dose-response curve for each enzyme using an ATP concentration of two-thirds Km for each. Most assays consist of enzyme mixed with kinase reaction buffer [20mM TrisHCl (pH 7.5),10mM MgCl2, 5mM MnCl2, 100mM NaCl, 1.5mM EGTA]. A final concentration of 1mM DTT, 0.2mM NaVO4, and 20μg/mL BSA is added before each assay. For all assays, 5.75mg/mL streptavidin-allophycocyanin and 0.1125nM Eu-PT66 are added immediately before the HTRF reaction. Plates are incubated for 30 minutes at room temperature and read on a Discovery instrument. IC50 values are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equation.   细胞实验:   Cells are preincubated for 2 hours with different concentrations of Motesanib, and exposed with 50 ng/mL VEGF or 20 ng/mL bFGF for an additional 72 hours. Cells are washed twice with DPBS, and plates are frozen at -70°C for 24 hours. Proliferation is assessed by the addition of CyQuant dye, and plates are read on a Victor 1420 workstation. IC50 data are calculated using the Levenberg-Marquardt algorithm into a four-parameter logistic equatio.   动物实验:   A431 cells are cultured in DMEM (low glucose) with 10% FBS and penicillin/streptomycin/glutamine. Cells are harvested by trypsinization, washed, and adjusted to a concentration of 5×107/mL in serum-free medium. Animals are challenged s.c.with 1×107 cells in 0.2mL over the left flank. Approximately 10 days thereafter, mice are randomized based on initial tumor.volume measurements and treated with either vehicle (Ora-Plus) or Motesanib. Tumor volumes and body weights arerecorded twice weekly and/or on the day of sacrifice. Tumor volume is measured with a Pro-Max electronic digital caliper and calculated using the formula length (mm)×width (mm)×height (mm) and expressed in mm3. Data are expressed as mean±SE.Repeated measures ANOVA followed by Scheffe post hoc testing for multiple comparisons is used to evaluate the statistical significance of observed differences.
保存条件：-20℃

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