A-674563 HCl

A-674563 HCl 是一种Akt抑制剂,在无细胞试验中Ki为11 nM,对PKA适度有效,作用于Akt1比作用于PKC选择性高30多倍。

A-674563 HCl Chemical Structure

A-674563 HCl Chemical Structure

CAS: 2070009-66-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) 3022.11 现货
2mg 1400.86 现货
5mg 2638.91 现货
100mg 22113 现货
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A-674563 HCl相关产品

相关信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
MIA PaCa cells Cytotoxic assay Cytotoxicity against human MIA PaCa cells by MTT assay, EC50=0.64 μM 17523610
MiaPaCa2 cell Proliferation assay Antiproliferative activity against human MiaPaCa2 cell line, EC50=0.4 μM 16678413
MOLM14 Cytotoxicity assay Cytotoxicity against human MOLM14 cells, EC50=0.06μM. 31207462
MV4-11 Cytotoxicity assay Cytotoxicity against human MV4-11 cells, EC50=0.092μM. 31207462
MOLM13 Cytotoxicity assay Cytotoxicity against human MOLM13 cells, EC50=0.17μM. 31207462
KB-3-1 Function assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 31515284
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 31515284
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for control Hh wild type fibroblast cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
点击查看更多细胞系数据

生物活性

产品描述 A-674563 HCl 是一种Akt抑制剂,在无细胞试验中Ki为11 nM,对PKA适度有效,作用于Akt1比作用于PKC选择性高30多倍。
特性 口服生物活性化合物(用苯基取代A-443654的吲哚基得到),比A-443654对Akt的选择性差。
靶点
Akt1 [1]
(Cell-free assay)
PKA [1]
(Cell-free assay)
CDK2 [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
ERK2 [1]
(Cell-free assay)
点击更多
11 nM(Ki) 16 nM(Ki) 46 nM(Ki) 110 nM(Ki) 260 nM(Ki)
体外研究(In Vitro)
体外研究活性

A-674563 HCl 是A-443654上的吲哚基被苯基取代的产物,具有口服活性。A-674563减慢肿瘤细胞的增殖,EC50为0.4 μM。[1] A-674563自身不会抑制Akt磷酸化,但是会剂量依赖性阻断Akt下游靶点的磷酸化。A-674563诱导的Akt阻塞会导致STS细胞下游靶点磷酸化下降和肿瘤细胞的生长抑制。A-674563诱导STS 细胞中G2细胞周期阻滞和细胞凋亡。[2]

激酶实验 Akt激酶试验
激酶试验使用His-Akt1和生物素化的小鼠Bad多肽作为底物。激酶试验在室温下,50 μL反应缓冲液[20 mM HEPES,pH 7.5,10 mM MgCl2,0.1% (w/v) Triton X-100,5 μM ATP (Km = 40 μM),5 μM 多肽(Km = 15 μM),1 mM DTT,60 ng Akt1,和0.5 μCi of [γ-33P]ATP]中,不同浓度A-674563存在下进行30分钟。每个反应通过加入50 μL终止缓冲液(0.1 M EDTA,pH 8.0,和4 M NaCl)停止。生物素化的Bad多肽固定在链霉亲和素包被的FLASH平板。用PBS-Tween 20 (0.05%)清洗后,FLASH 板上捕获的33P磷酸肽通过TopCount Packard Instruments γ计数器测量。
细胞实验 细胞系 MiaPaCa-2 细胞
浓度 0-30 μM
孵育时间 48小时
方法

将96孔板上的细胞用200 μL PBS缓慢清洗。Alamar Blue试剂以1:10在正常生长培养基中稀释。将稀释的Alamar Blue(100 M)加入到96孔板的每孔中,依据制造商的说明培养到反应完全。使用fmax荧光酶标仪进行分析,激发波长设置为544 nm,发射波长设置为595 nm。数据使用制造商提供的SOFTmax PRO软件分析。

体内研究(In Vivo)
体内研究活性

A-674563单一疗法没有显著的肿瘤抑制活性;与单独疗法相比,结合疗法的效能被显著提高。[1] A674563-处理的(20 mg/kg/bid, p.o.)小鼠体内肿瘤生长减慢,肿瘤体积减少50%,在研究结束时,与对照组相比。[2] A-674563被认为显著地提高了PK性能,在小鼠体内口服生物活性为67%,但是比A-443654的活性低70倍。[3]

动物实验 Animal Models 禁食小鼠
Dosages 20 或 100 mg/kg
Administration 1 g/kg葡萄糖刺激前30分钟给药A-674563

化学信息&溶解度

分子量 394.9 分子式

C22H22N4O.CIH

CAS号 2070009-66-2 SDF --
Smiles CC1=C2C=C(C=CC2=NN1)C3=CC(=CN=C3)OCC(CC4=CC=CC=C4)N
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 72 mg/mL ( (182.32 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : 72 mg/mL (182.32 mM)

Ethanol : 18 mg/mL (45.58 mM)

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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