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UM-164  ≥98%(HPLC)

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(5mg/mL)和水(10mg/mL)。
产品描述：基本信息 产品编号：U10020 产品名称：UM-164 CAS: 903564-48-7   储存条件 粉末 -20℃ 四年     分子式： C30H31F3N8O3S 溶于液体 -80℃ 六个月 分子量 640.69 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 100mg/mL (156.08mM) 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 1.5608mL 7.8042mL 15.6084mL 5mM 0.3122mL 1.5608mL 3.1217mL 10mM 0.1561mL 0.7804mL 1.5608mL 50mM 0.0312mL 0.1561mL 0.3122mL   生物活性 产品描述 一种有效的C-SRC/p38激酶抑制剂。 靶点/IC50 p38α p38β c-Src(Cell-free assay)     2.7nM(Kd)   体外研究 UM-164可与c-Src的非活性构象相结合。在TNBC细胞中，UM-164可改变c-Src的细胞定位，具有抗增殖活性，平均GI50=160nM。UM-164是p38α和p38β的有效抑制剂。在处理过50nM UM-164的SUM 149细胞中，p38 MAPK磷酸化完全消失。UM-164可抑制MDA-MB 231细胞和SUM 149细胞的运动和侵袭能力，IC50为50nM。在SUM 149细胞中，FAK磷酸化被UM-164抑制。UM-164还可有效地减少EGFR的激活（Tyr-845和Tyr-1068）、AKT及ERK1/2的激活，但这些都是不是UM-164的直接靶点。   体内研究 在TNBC(anti-triple-negative breast cancer)的异种移植瘤模型中，UM-164可显著地减少肿瘤生长，其体内毒性作用较小。   推荐实验方法(仅供参考) 细胞实验:   MDA-MB 231 and SUM 149 cells are plated in triplicate on 60mm dishes at a density of 1×106 cells/flask. After 24h, a final concentration of 1 µM UM-164 is added to the cells and incubated for 24h. Growth medium is then removed and cells are washed with PBS. The remaining cells are trypsinized, harvested, and placed together with growth medium and PBS. Cells are pelleted and re-suspended in 3mL of 75% ethanol, followed by overnight storage at -20°C. After incubation, cells are centrifuged at 1,500 rpm for 5 min and the cell pellets are re-suspended in 0.05mg/mL propidium iodide (10μg/mL) containing 300μg/mL RNase. Cell clumps are filtered. Cell DNA content is measured on flow cytometer and cell cycle distribution is calculated from 10,000 cells using FACS analysis.   动物实验:   Mice NCr/nude mice, 6 weeks of age,are anesthetized by injecting ketamine:xylazine combination at a concentration of 100mg/kg:10mg/kg. A total of 10,000 MDA-MB 231 cells are mixed with Matrigel in a 1:1 ratio by volume and injected into both left and right fourth mammary gland fat pads. Mice are randomized into treatment groups once the tumors are palpable. UM-164 is dissolved in a mixture of DMSO/propylene glycol (1:9). The volume of administration is 0.05mL/mouse. The control group receive 10 % DMSO/propylene glycol, and the treatment groups receive 10mg/kg, 15mg/kg, or 20mg/kg of UM-164. Mice are treated every other day by intraperitoneal injection, for up to 48 consecutive days. The tumors are monitored twice weekly, and body weight is measured once weekly. Tumor volume is calculated.
保存条件：-20℃

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