Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD-2461 是一种 PARP 抑制剂,可抑制 PARP1、PARP2 和 PARP3 的活性,IC50值分别为 5、2 和 200 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 457 | 现货 | ||
10 mg | ¥ 671 | 现货 | ||
50 mg | ¥ 1,232 | 现货 | ||
100 mg | ¥ 1,996 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 498 | 现货 |
产品描述 | AZD2461 is a novel PARP inhibitor. |
靶点活性 | PARP3:200 nM, PARP2:2 nM, PARP1:5 nM |
体外活性 | AZD2461在抗Olaparib的KB1P肿瘤T6-28上Mdr1b表达增加了80倍,没有抑制Pgp. |
体内活性 | AZD2461比奥拉帕尼对Pgp的亲和力低。 |
激酶实验 | ELISA-Based ERBB Kinase Assay: The ERBB1, ERBB 2, and ERBB4 cytoplasmic fusion proteins are made by cloning the ERBB1 sequence (Met-668 to Ala-1211), ERBB2 (Ile-675 to Val-1256), and ERBB4 sequence (Gly-259 to Gly-690) into the baculoviral vector pFastBac using PCR. Proteins are expressed in baculovirusinfected Sf9 insect cells as GST fusion proteins. The proteins are purified by affinity chromatography using glutathione sepharose beads. Inhibition of ERBB tyrosine kinase activity is assessed using an ELISA-based receptor tyrosine kinase assay. Kinase reactions (50 mM HEPES, pH 7.4, 125 mM NaCl, 10 mM MgCl2, 100 μM sodium orthovanadate, 2 mM dithiothreitol, 20 μM ATP, PF299804 or vehicle control, and 1-5 nM GST-erbB per 50 μL of reaction mixture) are run in 96-well plates coated with 0.25 mg/mL poly-Glu-Tyr. The reactions are incubated for 6 minutes at room temperature while being shaken. Kinase reactions are stopped by removal of the reaction mixture, and then the wells are washed with wash buffer (0.1% Tween 20 in PBS). Phosphorylated tyrosine residues are detected by adding 0.2 μg/mL antiphosphotyrosine antibody (Oncogene Ab-4; 50 μL/well) coupled to horseradish peroxidase (HRP) diluted in PBS containing 3% BSA and 0.05% Tween 20 for 25 minutes while being shaken at room temperature. The antibody is removed, and plates are washed in wash buffer. HRP substrate (SureBlue3,3?,5,5?-tetramethyl benzidine or TMB) is added (50 μL per well) and incubated for 10-20 minutes while it is shaken at room temperature. The TMB reaction is stopped with the addition of 50 μL of stop solution (0.09 N H2SO4). The signal is quantified by measuring absorbance at 450 nm. IC50 values are determined for PF299804 using the median effect method. |
分子量 | 395.43 |
分子式 | C22H22FN3O3 |
CAS No. | 1174043-16-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 39.5 mg/mL (100 mM)
Ethanol: 39.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.5289 mL | 12.6445 mL | 25.2889 mL | 63.2223 mL |
5 mM | 0.5058 mL | 2.5289 mL | 5.0578 mL | 12.6445 mL | |
10 mM | 0.2529 mL | 1.2644 mL | 2.5289 mL | 6.3222 mL | |
20 mM | 0.1264 mL | 0.6322 mL | 1.2644 mL | 3.1611 mL | |
50 mM | 0.0506 mL | 0.2529 mL | 0.5058 mL | 1.2644 mL | |
100 mM | 0.0253 mL | 0.1264 mL | 0.2529 mL | 0.6322 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。
AZD-2461 1174043-16-3 Chromatin/Epigenetic DNA Damage/DNA Repair PARP Inhibitor inhibit AZD 2461 AZD2461 poly ADP ribose polymerase inhibitor