SKI V  ≥98%

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包装规格:1mg 5mg 10mg in glass bottle
溶解性:溶于DMSO(250 mg/mL 超声)
产品描述:基本信息 产品编号: S10715 产品名称: SKI V CAS: 24418-86-8   储存条件 粉末 -20℃ 四年     分子式: C15H10O4 溶于液体 -80℃ 6个月 分子量: 254.24 -20℃ 1个月 化学名:  2-(3,4-Dihydroxy-benzylidene)-benzofuran-3-one,Sphingosine Kinase Inhibitor V Solubility (25°C):   体外:   DMSO 51mg/mL (200.59mM) 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 3.9333mL 19.6665mL 39.3329mL 5mM 0.7867mL 3.9333mL 7.8666mL 10mM 0.3933mL 1.9666mL 3.9333mL 50mM 0.0787mL 0.3933mL 0.7867mL   生物活性 产品描述 一种非竞争性的,有效的非脂质鞘氨醇激酶(SPHK;SK)抑制剂,对GST-hSK的IC50为2μM。 靶点 GST-hSK  hPI3k  2μM 6μM   体外研究 SKI V has weak activity toward ERK2 (IC50 of 80μM for hERK2) and does not inhibit PKC-α.SKI V (10μM;for 24 hours) inhibits cancer cell proliferation and induces apoptosis.SKI V (0.2,1,5μM;pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels.Near-confluent cultures of JC cells are serum-starved for 16 hours,followed by pretreatment SKI V for 1 hour.SKI V has IC50s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of -2μM.SKI V (20μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells.SKI V (0.2,1,5μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion. Cell Proliferation Assay Cell Line: T24 tumor cells Concentration: 10μM Incubation Time: For 24 hours Result: Inhibited cancer cell proliferation. Apoptosis Analysis Cell Line: T24 tumor cells Concentration: 10μM Incubation Time: For 24 hours Result: Induced apoptosis. Western Blot Analysis Cell Line: JC cells Concentration: 0.2,1,5μM Incubation Time: Pretreated for 1 hour Result: Decreased phospho-Akt and phospho-MEK levels. 体内研究 SKI V (75mg/kg;i.p.;days 1,5,9,15) significantly lowers tumor growth (>50% decreased at day 18) than control animals. Animal Model: 6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells Dosage: 75mg/kg Administration: IP;days 1,5,9,15 Result: Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.
保存条件:-20℃