Powder: -20°C for 3 years | In solvent: -80°C for 1 year
KRCA-0008 是高效的、选择性的 ALK/Ack1 抑制剂,对ALK 和Ack1的IC50值分别为12nM 和4nM,显示出非hERG 依赖性药物活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 206 | 现货 | ||
5 mg | ¥ 538 | 现货 | ||
10 mg | ¥ 913 | 现货 | ||
25 mg | ¥ 1,630 | 现货 | ||
50 mg | ¥ 3,220 | 现货 | ||
100 mg | ¥ 4,770 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 555 | 现货 |
产品描述 | KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability. |
靶点活性 | Ack1:4 nM, ALK:12 nM |
激酶实验 | Assay of Abl1 kinase isoforms and determination of inhibitor potency: Activity of u-Abl1native is determined by following the production of ADP from the kinase reaction through coupling with the pyruvate kinase/lactate dehydrogenase system. In this assay, the oxidation of NADH (measured as a decreased A340 nM) is continuously monitored spectrophotometrically. The final reaction mixture (100 μL, in a 384-well Corning plate) is prepared as follows: An Abl1 kinase/coupled assay components mixture is prepared containing u-Abl1 kinase (1 nM), Abltide (EAIYAAPFAKKK, 0.2 mM), MgCl2 (9 mM), pyruvate kinase (~ 4 units), lactate dehydrogenase (~ 0.7 units), phosphoenol pyruvate (1 mM), and NADH (0.28 mM) in 90 mM Tris containing 0.1 % octyl-glucoside and 1 % DMSO, pH 7.5. Separately, an inhibitor mixture is prepared containing DCC-2036 serially diluted 3-fold in DMSO followed by dilution into buffer composed of 180 mM Tris, pH 7.5, containing MgCl2 (18 mM) and 0.2 % octyl-glucoside. Fifty μL of the inhibitor mixture is mixed with 50 μL of the above Abl1 kinase/coupled assay components mixture, which is then incubated at 30 °C for 2 hours before 2 μL of 25 mM ATP (500 μM, final) is added to start the reaction. The reaction is recorded every 2 minutes for 2.5 hours at 30 °C on a Polarstar Optima or Synergy2 plate reader. Reaction rate (slope) is calculated using the 1 to 2 hour time frame with reader's software. Percent inhibition is obtained by comparison of reaction rate with that of a DMSO control. IC50 values are calculated from a series of percent inhibition values determined at a range of inhibitor concentrations using GraphPad Prism. The kinase assay for Abl1T315I, p-Abl1native or Abl1H396P is assayed the same as above except that 2.2 nM Abl1T315I, 1 nM p-Abl1 native or 1.3 nM Abl1H396P is used. The above assay format is also used for kinases other than Abl1 with the exception of TIE2, for which a fluorescence polarization/Transcreener format is used.The assay conditions are the same as described above except that PolyE4Y (final 1 mg/mL) is used as the substrate and one hour preincubation is used. |
别名 | KRCA 0008, KRCA0008 |
分子量 | 609.12 |
分子式 | C30H37ClN8O4 |
CAS No. | 1472795-20-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12 mg/mL (19.7 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.6417 mL | 8.2086 mL | 16.4171 mL | 41.0428 mL |
5 mM | 0.3283 mL | 1.6417 mL | 3.2834 mL | 8.2086 mL | |
10 mM | 0.1642 mL | 0.8209 mL | 1.6417 mL | 4.1043 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。
KRCA-0008 1472795-20-2 Angiogenesis Tyrosine Kinase/Adaptors ACK ALK selective crizotinib Ack1 inhibit diaminopyrimidine analogue TNK2 ALCL N-Acetylpiperidine KRCA 0008 Anaplastic lymphoma kinase (ALK) KRCA0008 cell cycle arrest Anaplastic lymphoma kinase apoptosis Inhibitor ALK tyrosine kinase receptor CD246 Activated Cdc42 kinase 1 Cluster of differentiation 246 inhibitor