化合物 A-674563|T6139|TargetMol

A-674563
552325-73-2

￥483 1mg 起订

￥1160 5mg 起订

￥1820 10mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 化合物 A-674563

英文名称：: A-674563

CAS号：: 552325-73-2

品牌：: TargetMol

产地：: 美国

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

纯度规格：: 99.21%

产品类别：: 抑制剂

货号：: T6139

Product Introduction

Bioactivity

Name	A-674563
Description	A-674563 is an Akt1 inhibitor with Ki of 11 nM, modest potent to PKA and >30-fold selective for Akt1 over PKC.
Cell Research	The cells on 96-well plates are gently washed with 200 μL of PBS. Alamar Blue reagent is diluted 1:10 in normal growth media. The diluted Alamar Blue reagent (100 M) is added to each well on the 96-well plates and incubated until the reaction is complete as per manufacturer's instructions. Analysis is done using an fmax Fluorescence Microplate Reader, set at the excitation wavelength of 544 nm and emission wavelength of 595 nm. Data are analyzed using SOFTmax PRO software provided by the manufacturer. (Only for Reference)
Kinase Assay	Akt Kinase Assay: The kinase assay uses His-Akt1 and a biotinylated mouse Bad peptide as substrate. The kinase assay is carried out at room temperature for 30 minutes in 50 μL of reaction buffer [20 mM HEPES, pH 7.5, 10 mM MgCl2, 0.1% (w/v) Triton X-100, 5 μM ATP (Km = 40 μM), 5 μM peptide (Km = 15 μM), 1 mM DTT, 60 ng of Akt1, and 0.5 μCi of [γ-33P]ATP] in the presence of different concentrations of A-674563. Each reaction is stopped by adding 50 μL of termination buffer (0.1 M EDTA, pH 8.0, and 4 M NaCl). The biotinylated Bad peptides are immobilized on streptavidin-coated FLASH plates. After being washed with PBS-Tween 20 (0.05%), the 33P phosphopeptide captured on the FLASH plates is measured with a TopCount Packard Instruments γ counter.
In vitro	A-674563是通过将A-443654中的吲哚基团替换为苯基团并获得口服活性而得到的。A-674563能够以0.4μM的EC50抑制肿瘤细胞的增殖。[1] A-674563本身不抑制Akt的磷酸化，但能以剂量依赖性方式阻断Akt下游靶点的磷酸化。A-674563引起的Akt阻断导致STS细胞下游靶点磷酸化减少以及肿瘤细胞生长抑制。A-674563在STS细胞中诱导G2细胞周期阻滞及凋亡。[2]
In vivo	在口服葡萄糖耐量测试中，20 mg/kg A-674563可提高血浆胰岛素水平。A-674563单药治疗未显示出明显的抑瘤活性；与紫杉醇单药治疗相比，联合治疗的疗效显著提高。[1]治疗的小鼠（20 mg/kg/bid，p.o.）展现出比对照组更慢的肿瘤生长速率，并在研究终点时肿瘤体积减少了50%以上。[2]在小鼠中，A-674563的口服生物利用度为67%，其药代动力学（PK）特性显著提高，但其活性比A-443654低70倍。[3]
Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	H2O : 66 mg/mL (184.1 mM) DMSO : 67 mg/mL (186.9 mM) Ethanol : 15 mg/mL (41.8 mM)
Keywords	Protein kinase B \| PKB \| inhibit \| Akt \| A-674563 \| A 674563 \| Inhibitor
Inhibitors Related	Lidocaine hydrochloride \| Astragaloside IV \| Lidocaine \| Sodium Oxamate \| Ribociclib \| 4-Chloro-2'-bromoacetophenone \| Tauroursodeoxycholate \| Artemisinin \| Acefylline \| 2,3-Butanediol \| TBHQ \| Abemaciclib
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| Pain-Related Compound Library

A674563|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。

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