生物试剂
>
生化试剂
>
信号通路
> PHA-665752
加入收藏 取消收藏

PHA-665752  ≥98%

促销价¥{{model.attbuying.price}}

市场价¥0.00

累计销量0 累计评价0 人评论

别称 {{model.alias}}
中文名称 {{model.name}}
英文名称 {{model.enname}}
品牌 {{model.brand}}
CAS {{model.cas}}
分子式
分子量 {{model.molecularweight}}
MDL {{model.mdl}}
货号 {{model.procode}}
数量

+ -

件 库存{{model.attbuying.number}}件
立即购买 加入购物车 下载说明书

看了又看
包装规格：5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（50 mg/mL 超声）
产品描述：基本信息 产品编号：P10801 产品名称：PHA-665752 CAS: 477575-56-7   储存条件 粉末 -20℃ 四年     分子式： C32H34Cl2N4O4S 溶于液体 -80℃ 六个月 分子量 641.61 -20℃ 一个月 化学名：      Solubility (25°C)   体外 DMSO 128mg/mL (199.49mM) Ethanol Insoluble Water Insoluble 体内（现配现用） 2% DMSO+castor oil 5mg/mL ＜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 1.5586mL 7.7929mL 15.5858mL 5mM 0.3117mL 1.5586mL 3.1172mL 10mM 0.1559mL 0.7793mL 1.5586mL 50mM 0.031mL 0.1559mL 0.3117mL   生物活性 产品描述 一种选择性的 ATP 竞争活性位点 c-Met 激酶抑制剂，Ki 为 4nM，IC50为 9nM。 靶点/IC50 Ki: 4nM IC50: 9nM (c-Met)   体外研究 PHA-665752 is a potent and ATP-competitive inhibitor of c-Met kinase activity with a Ki of 4nM and an IC50 of 9 nM.PHA-665752 exhibits >50-fold selectivity for c-Met enzyme compared with the majority of kinases evaluated.PHA-665752 shows potent inhibition of c-Met RTK autophosphorylation in NIH3T3 cells engineered to express high levels of c-Met and hepatocyte growth factor (HGF).PHA-665752 inhibits HGF-stimulated or constitutive phosphorylation of mediators of downstream of c-Met such as Gab-1,ERK, Akt, STAT3, PLC-γ, and FAK in multiple tumor cell lines.PHA-665752 (0-1.25μM; 18 hours) potently inhibits HGF and Met-driven phenotypes such as cell growth (proliferation and survival), cell motility, invasion, and/or morphology of a variety of tumor cells.PHA-665752 (0-1.25μM; 72 hours) induces apoptosis in both the presence and absence of HGF at concentrations that nhibited tyrosine phosphorylation of c-Met in GTL-16 cells.PHA-665752 (0.0125-0.2 μM; 4 hours) potent inhibits HGF-induced c-Met phosphorylation in A549 cells.Cell Proliferation Assay Cell Line: S114 cells, GTL-16 cells, NCI-H441 cells, or BxPC-3 cells Concentration: 0 μM,0.002μM,0.01μM,0.05μM,0.25μM, 1.25μM Incubation Time: 18 hours Result: Potently inhibited HGF and c-Met-driven cell growth.   Apoptosis Analysis Cell Line: GTL-16 cells Concentration: 0μM,0.002μM,0.01μM,0.05μM,0.25μM,1.25μM Incubation Time: 72 hours Result: Induced apoptosis in both the presence and absence of HGF at concentrations that inhibited tyrosine phosphorylation of c-Met in GTL-16 cells. Immunoblot Analysis. Western Blot Analysis Cell Line: A549 cells Concentration: 0.0125μM,0.025μM,0.05μM,0.1μM,0.2μM Incubation Time: 4 hours Result: Potent inhibited HGF-induced c-Met phosphorylation in A549 cells. 体内研究 PHA-665752 (7.5-30mg/kg/day; i.v. ; for 9 days) exhibits statistically significant dose-dependent tumor growth inhibition of 68%, 39%, and 20% of vehicle control at the 30mg/kg/day,15mg/kg/day, and 7.5mg/kg/day doses,respectively.PHA-665752 shows a potent cytoreductive activity in a gastric carcinoma xenograft model. Animal Model: Female athymic mice (nu/nu, 8–12 weeks) bearing S114 or GTL-16 tumor xenografts Dosage: 7.5mg/kg/day, 15mg/kg/day, 30mg/kg/day Administration: Intravenous injection; for 9 days Result: Demonstrated statistically significant dose-dependent tumor growth inhibition.   推荐实验方法(仅供参考) 激酶实验： 体外酶实验 使用GST融合蛋白的c-Met激酶域进行c-Met实验。在ATP和二价阳离子 (MgCl2 或 MnCl2 10-20mM)存在时，根据激酶肽底物和聚-glu-tyr的磷酸化，测定PHA-665752抑制c-Met的IC50值。测定作用于c-Met的线性范围(即,速率维持初始速率的时间周期), 然后在这个范围内测定动力学和IC50值。   细胞实验:   细胞系 S114, GTL-16, NCI-H441, 和 BxPC-3 浓度 溶于DMSO, 终浓度为~10μM 处理时间 18,或72小时 方法 增殖实验中, 细胞生长在含0.1% FBS 的培养基中48小时， 然后使用不同浓度PHA-665752处理细胞。18小时后,细胞和BrdUrd温育1小时，混合，使用抗BrdUrd过氧化物酶抗体染色,然后实验板在630nm处读数。凋亡实验中, 细胞生长在含2% FBS的培养基中，在有或无HGF (50ng/mL) 存在时，使用不同浓度PHA-665752处理细胞72小时。72小时后, 加入含溴化乙锭和吖啶橙的混合物,通过荧光显微镜计算凋亡细胞(明亮的橙色细胞或细胞碎片)。   动物实验:   动物模型 携带S114 或GTL-16移植瘤的雌性无胸腺nu/nu小鼠 剂量 ~30mg/kg/day 给药处理 静脉注射
保存条件：-20℃

猜你喜欢