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
CAS: 2070009-66-2
产品质控
批次：
纯度：
99.66%
99.66
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 |
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| 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] |
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|---|---|---|---|---|
| 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。 |
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| 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] |
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|---|---|---|
| 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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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
只
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，注：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：取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：取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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