化合物 KRCA-0008|T2641|TargetMol

KRCA-0008
1472795-20-2

￥186 1mg 起订

￥258 2mg 起订

￥413 5mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 KRCA-0008

英文名称：: KRCA-0008

CAS号：: 1472795-20-2

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 98.43%

产品类别：: 抑制剂

货号：: T2641

Product Introduction

Bioactivity

名称	KRCA-0008
描述	KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability.
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 \| Shipping with blue ice.
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	Vemurafenib \| Crizotinib \| RepSox \| Ceritinib \| A 83-01 \| Lorlatinib \| ALK-IN-1 \| EML4-ALK kinase inhibitor 1 \| Alectinib hydrochloride \| SB-431542 \| LDN-193189 2HCl \| DMH-1
相关库	抑制剂库 \| 经典已知活性库 \| 抗癌化合物库 \| 已知活性化合物库 \| 激酶抑制剂库 \| NO PAINS 化合物库 \| 抗肺癌化合物库 \| 膜蛋白靶向化合物库 \| 酪氨酸激酶分子库 \| 表型筛选靶点鉴定库

KRCA 0008|||KRCA0008|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
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主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务