化合物KRCA-0008 T2641
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 1472795-20-2 | ¥3,290.00 | 询底价 |
50 mg | 1472795-20-2 | ¥1,990.00 | 询底价 |
10 mg | 1472795-20-2 | ¥579.00 | 询底价 |
1 mL | 1472795-20-2 | ¥553.00 | 询底价 |
2 mg | 1472795-20-2 | ¥258.00 | 询底价 |
5 mg | 1472795-20-2 | ¥413.00 | 询底价 |
25 mg | 1472795-20-2 | ¥1,160.00 | 询底价 |
1 mg | 1472795-20-2 | ¥186.00 | 询底价 |
Product Introduction
Bioactivity
英文名: KRCA-0008
描述: 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。
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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 12 mg/mL (19.7 mM)
关键字: selective | crizotinib | Ack1 | inhibit | diaminopyrimidine | analogue | TNK2 | ALCL | N-Acetylpiperidine | Anaplastic lymphoma kinase (ALK) | cell cycle arrest | KRCA-0008 | Anaplastic lymphoma kinase | apoptosis | Inhibitor | ALK tyrosine kinase receptor | CD246 | Activated Cdc42 kinase 1 | Cluster of differentiation 246
相关产品: GNF-7 | Vemurafenib | AIM-100 | AZ7550
相关库: Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Anti-Lung Cancer Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途