Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PI-273 是一种可逆的特异性磷脂酰肌醇 4-激酶抑制剂,IC50为 0.47 μM。它可抑制乳腺癌细胞的增殖,阻断细胞周期并诱导细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 652 | 现货 | ||
5 mg | ¥ 1,320 | 现货 | ||
10 mg | ¥ 2,230 | 现货 | ||
25 mg | ¥ 3,850 | 现货 | ||
50 mg | ¥ 5,520 | 现货 | ||
100 mg | ¥ 7,730 | 现货 | ||
500 mg | ¥ 15,300 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,590 | 现货 |
产品描述 | PI-273, a Substrate-Competitive, Specific Small-Molecule Inhibitor of PI4KIIα, Inhibits the Growth of Breast Cancer Cells |
靶点活性 | PI4KIIα:0.47 μM |
体外活性 | PI-273 exhibited the greatest inhibitory effect on PI4KIIα kinase activity (IC50 = 0.47 μmol/L) and suppressed cell proliferation.?Surface plasmon resonance and thermal shift assays indicated that PI-273 interacted directly with PI4KIIα.?The kinetic analysis identified PI-273 as a reversible competitive inhibitor with respect to the substrate phosphatidylinositol (PI), which contrasted with most other PI kinase inhibitors that bind the ATP binding site.?PI-273 reduced PI4P content, cell viability, and AKT signaling in wild-type MCF-7 cells, but not in PI4KIIα knockout MCF-7 cells, indicating that PI-273 is highly selective for PI4KIIα.?Mutant analysis revealed the role of palmitoylation insertion in the selectivity of PI-273 for PI4KIIα.?In addition, PI-273 treatment retarded cell proliferation by blocking cells in G2-M, inducing cell apoptosis and suppressing colony-forming ability.?Importantly, PI-273 significantly inhibited MCF-7 cell-induced breast tumor growth without toxicity.?PI-273 is the first substrate-competitive, a subtype-specific inhibitor of PI4KIIα, the use of which will facilitate evaluations of PI4KIIα as a cancer therapeutic target. |
体内活性 | PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts[1].PI-273 (0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%[1]. |
分子量 | 381.9 |
分子式 | C16H16ClN3O2S2 |
CAS No. | 925069-34-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 6 mg/mL (15.71 mM), ultrasonic and warming and heat to 60°C
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6185 mL | 13.0924 mL | 26.1849 mL | 65.4622 mL |
5 mM | 0.5237 mL | 2.6185 mL | 5.237 mL | 13.0924 mL | |
10 mM | 0.2618 mL | 1.3092 mL | 2.6185 mL | 6.5462 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。
PI-273 925069-34-7 Apoptosis PI3K/Akt/mTOR signaling PI4K Inhibitor PI4 kinases PI 273 inhibit Phosphatidylinositol 4 kinases PI273 inhibitor