Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PIK90 PIK-90 是一种 DNA-PK 和 PI3K 抑制剂,抑制 p110α、p110γ和DNA-PK,IC50分别为 11、18 和 13 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 196 | 现货 | ||
5 mg | ¥ 435 | 现货 | ||
10 mg | ¥ 717 | 现货 | ||
25 mg | ¥ 1,290 | 现货 | ||
50 mg | ¥ 2,260 | 现货 | ||
100 mg | ¥ 3,570 | 现货 | ||
200 mg | ¥ 4,970 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 528 | 现货 |
产品描述 | PIK-90, a DNA-PK and PI3K inhibitor, suppresses p110α( IC50=11 nM), p110γ(IC50=18 nM) and DNA-PK(IC50=13 nM) . |
靶点活性 | PI3Kγ:18 nM, PI3Kα:11 nM, DNA-PK:13 nM |
体外活性 | 胰岛素刺激的动物,PIK-90(10 mg/kg)处理,能够抑制由胰岛素刺激产生的血糖降低. |
体内活性 | 在慢性淋巴细胞白血病细胞中,PIK-90(1-10 μM )处理,抑制趋化性,明显抑制细胞迁移进入基质细胞层,降低CXCL12诱导的肌动蛋白聚合。在dHL60细胞中,PIK-90抑制fMLP刺激的Akt磷酸化,损害极性和趋化性。在胶质瘤细胞系中(U87 MG, SF188, SF763, LN229, A1207和LN-Z30细胞),PIK-90阻断Akt磷酸化,抑制细胞增殖。 |
激酶实验 | Expression and Assay of p110α/p85α, p110β/p85α, p110δ/p85α, and p110γ : IC50 values are measured using either a standard TLC assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 μM or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements. |
细胞实验 | For viabilty, cells are seeded in 12-well plates in the presence of PIK-90 for 3 days. Cell viability is determined using a WST-1 assay.(Only for Reference) |
分子量 | 351.36 |
分子式 | C18H17N5O3 |
CAS No. | 677338-12-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.51 mg/ml (10 mM), Sonification is recommended
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8461 mL | 14.2304 mL | 28.4608 mL | 71.1521 mL |
5 mM | 0.5692 mL | 2.8461 mL | 5.6922 mL | 14.2304 mL | |
10 mM | 0.2846 mL | 1.423 mL | 2.8461 mL | 7.1152 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PIK-90 677338-12-4 DNA Damage/DNA Repair PI3K/Akt/mTOR signaling DNA-PK PI3K Inhibitor PIK90 Phosphoinositide 3-kinase DNA-dependent protein kinase PIK 90 inhibit inhibitor