Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CNX1351 是有效的、选择性的 PI3Kα 抑制剂,其 IC50=6.8 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 425 | 现货 | ||
5 mg | ¥ 946 | 现货 | ||
10 mg | ¥ 1,580 | 现货 | ||
25 mg | ¥ 3,130 | 现货 | ||
50 mg | ¥ 4,670 | 现货 | ||
100 mg | ¥ 6,650 | 现货 | ||
500 mg | ¥ 13,300 | 现货 |
产品描述 | CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor. |
靶点活性 | PI3Kα:6.8 nM |
激酶实验 | Biochemistry assay: The motor domains of KSP (amino acids 1–360) is expressed as in Escherichia coli BL21(DE3) as COOH-terminal 6-his fusion proteins. Bacterial pellets are lysed in a microfluidizer with a lysis buffer [50 mM Tris-HCl; 50 mM KCl, 10 mM imidazole, 2 mM MgCl2, 8 mM β-mercaptoethanol, 0.1 mM ATP (pH 7.4)], and proteins are purified using Ni-NTA agarose affinity chromatography, with an elution buffer consisting of 50 mM PIPES, 10% sucrose, 300 mM imidazole, 50 mM KCl, 2 mM MgCl2, mM β-mercaptoethanol, and 0.1 mM ATP (pH 6.8). Steady-state measurements of ATPase activity are performed with a pyruvate kinase–lactate dehydrogenase detection system that coupled the appearance of ADP with oxidation of NADH. Absorbance changes are monitored at 340 nm. All biochemical experiments are performed in PEM25 buffer [25 mM Pipes/KOH (pH 6.8), 2 mM MgCl2, 1 mM EGTA] supplemented with 10 μM SB 743921 for experiments involving microtubules. Rates of ADP release are measured in a stopped-flow apparatus; the decrease in fluorescence of MANT-ATP is monitored. Rates of Pi release are measured in a stopped-flow apparatus, using bacterial phosphate binding protein modified with 7-diethylamino-3-((((2 maleimidyl)ethyl)amino)carbonyl)coumarin (MDCC) dye. Ki estimates of KSP inhibitors are extracted from the dose–response curves, with explicit correction for enzyme concentration. Tubulin polymerization by measuring changes in absorbance at 340 nm is monitored. The assay is performed in 100-μL volumes in 96-well half-area microtiter plates, using a microplate reader with the incubation temperature set at 37 °C. |
别名 | 1-[4-[[2-(1H-吲唑-4-基)-4-(4-吗啉基)噻吩并[3,2-D]嘧啶-6-基]甲基]-1-哌嗪基]-6-甲基-5-庚烯-1,4-二酮 |
分子量 | 573.71 |
分子式 | C30H35N7O3S |
CAS No. | 1276105-89-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 5.73 mg/mL (9.99 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.743 mL | 8.7152 mL | 17.4304 mL | 43.576 mL |
5 mM | 0.3486 mL | 1.743 mL | 3.4861 mL | 8.7152 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。
CNX-1351 1276105-89-5 PI3K/Akt/mTOR signaling PI3K CNX 1351 inhibit 1-[4-[[2-(1H-吲唑-4-基)-4-(4-吗啉基)噻吩并[3,2-D]嘧啶-6-基]甲基]-1-哌嗪基]-6-甲基-5-庚烯-1,4-二酮 Phosphoinositide 3-kinase CNX1351 Inhibitor inhibitor