A-674563 HCl

目录号：S2670 Purity: 99.66%

A-674563 HCl 是一种Akt抑制剂，在无细胞试验中K_i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

规格	价格	库存
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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产品质控

批次：纯度： 99.66%

99.66

A-674563 HCl相关产品

相关靶点	Akt1 Akt2 Akt3	点击展开
相关产品	MK-2206 2HCl Perifosine SC79 Capivasertib (AZD5363) GSK690693 Ipatasertib (GDC-0068) Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) AT13148 Miransertib (ARQ 092) HCl Uprosertib (GSK2141795) Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库凋亡分子化合物库细胞周期化合物库 NF-κB信号通路库	点击展开

细胞实验数据示例

细胞系	实验类型	活性描述	文献信息(PMID)
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K_i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)	点击更多

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
激酶实验	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 (K_m = 40 μM)，5 μM 多肽(K_m = 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

参考文献
https://pubmed.ncbi.nlm.nih.gov/15956255/ https://pubmed.ncbi.nlm.nih.gov/20582381/ http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2932704/

参考文献

https://pubmed.ncbi.nlm.nih.gov/15956255/
https://pubmed.ncbi.nlm.nih.gov/20582381/
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2932704/

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

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)

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

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	Saline 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	30.000mg/ml (75.97mM)	以 1 mL 工作液为例，取30mg该产品加到1ml生理盐水（0.9% NaCL溶液）中，混合均匀使其澄清，请现配现用！
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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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