AT9283

AT9283是一种有效的JAK2/3抑制剂,无细胞试验中IC50为1.2 nM/1.1 nM;对Aurora A/B,Abl1(T315I)也有效。

AT9283 Chemical Structure

AT9283 Chemical Structure

CAS: 896466-04-9

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2444.92 现货
2mg RMB 818.33 现货
5mg RMB 1380.26 现货
50mg RMB 6298.93 现货
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客户使用Selleck的AT9283发表文献29

客户使用该产品的3个实验数据

产品质控

批次: 纯度: 100%
100

AT9283相关产品

相关信号通路图

JAK抑制剂选择性比较

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
Sf9 Function assay 10 uM 60 mins Displacement of BODIPY-ATP from C-terminal thrombin-cleavable hexa-histidine tagged human JAK2 JH2 pseudokinase domain (536 to 812 residues) W659A/W777A/F794H mutant expressed in baculovirus-infected Sf9 cells at 10 uM after 60 mins by high-throughput flu 28626521
HCT116 Function assay 20 mg/kg Cmax in BALB/c mouse bearing human HCT116 cells at 20 mg/kg, ip, Cmax=8.4μM 19143567
HCT116 Function assay 5 mg/kg Cmax in BALB/c mouse bearing human HCT116 cells at 5 mg/kg, iv, Cmax=4.9μM 19143567
HCT116 Function assay 10 mg/kg Cmax in BALB/c mouse bearing human HCT116 cells at 10 mg/kg, po, Cmax=0.45μM 19143567
HCT116 Cytotoxicity assay 10 to 14 days Cytotoxicity against human HCT116 cells assessed as number of colonies after 10 to 14 days by colony forming assay, IC50=0.012μM 19143567
HT-29 Antitumor assay 72 hrs Antitumor activity against human HT-29 cells after 72 hrs by MTT assay, IC50=0.383μM 23664099
A549 Antitumor assay 72 hrs Antitumor activity against human A549 cells after 72 hrs by MTT assay, IC50=0.512μM 23664099
LoVo Antitumor assay 72 hrs Antitumor activity against human LoVo cells after 72 hrs by MTT assay, IC50=0.553μM 23664099
K562 Antitumor assay 72 hrs Antitumor activity against human K562 cells after 72 hrs by MTT assay, IC50=1.6μM 23664099
U937 Antitumor assay 72 hrs Antitumor activity against human U937 cells after 72 hrs by MTT assay, IC50=6.7μM 23664099
BL21 (DE3) Function assay 30 mins Inhibition of His6-tagged MELK catalytic domain (1 to 340 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) cells using Bcl-GL as substrate measured after 30 mins in presence of [gamma32P]ATP by liquid scintillation counting method, IC50=0.685μM 28351607
Sf9 Function assay Binding affinity to N-terminal TEV-cleavable hexa-histidine tagged human JAK2 JH1 domain (840 to 1132 residues) expressed in baculovirus-infected Sf9 cells by ITC assay, Kd=0.011μM 28626521
Sf9 Function assay Binding affinity to C-terminal thrombin-cleavable hexa-histidine tagged human JAK2 JH2 pseudokinase domain (536 to 812 residues) W659A/W777A/F794H mutant expressed in baculovirus-infected Sf9 cells by ITC assay, Kd=1.323μM 28626521
HCT116 Function assay Inhibition of Aurora B kinase in human HCT116 cells assessed as reduction in polyploid phenotype, IC50=0.03μM 28918096
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
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
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS 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
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 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
fibroblast cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 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
点击查看更多细胞系数据

生物活性

产品描述 AT9283是一种有效的JAK2/3抑制剂,无细胞试验中IC50为1.2 nM/1.1 nM;对Aurora A/B,Abl1(T315I)也有效。
特性 AT9283是有效的pan-aurora 抑制剂。
靶点
JAK3 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
Aurora A [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
Abl1 (T315I) [1]
(Cell-free assay)
点击更多
1.1 nM 1.2 nM ~3.0 nM ~3.0 nM 4 nM
体外研究(In Vitro)
体外研究活性

在体外, AT9283有效抑制多种激酶,包括 Aurora A, Aurora B, JAK3, JAK2和 Abl,IC50分别为3 nM, 3 nM, 1.1 nM, 1.2 nM 和 4 nM。AT9283 作用于HCT116 细胞,通过抑制Aurora B 激酶活性,产生明显的多倍体表现型,IC50为30 nM。而且, AT9283也有效抑制HCT116形成集落。[1]

激酶实验 Aurora A和 Aurora B激酶实验
在DELFIA格式中进行Aurora A 和 B实验。Aurora A 酶和AT9283 及 3 μM 肽底物 (生物素-CGPKGPGRRGRRRTSSFAEG)在 10 mM MOPS, pH 7, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% 甘油, 0.2 mM EDTA, 10 mM MgCl2, 0.01% β-巯基乙醇, 15 μM ATP,和2.5% DMSO混合物中温育。Aurora B 酶和AT9283,及3 μM 以上底物在25 mM Tris, pH 8.5, 5 mM MgCl2, 0.1 mg/mL BSA, 0.025% Tween-20, 1 mM DTT, 15 μM ATP, 和 2.5% DMSO的混合物中温育。Aurora A 和 Aurora B反应分别进行60分钟和45-90分钟,然后使用 EDTA进行淬火。反应混合物转移到亲和素包被的实验板上,通过时间分辨荧光技术(激发波长, 337 nm;发射波长, 620 nm),使用特定磷酸抗体和铕标记的二抗测量磷酸化的肽。
细胞实验 细胞系 HCT 116 细胞
浓度 1 nM 到10 μM
孵育时间 72 小时
方法

HCT 116细胞培养在DMEM +10% FBS + GLUTAMAX I 中。细胞接种在黑色96孔平底组织培养板中,孔中含200 μL 培养基,在37oC 下温育约16小时,在湿润且含5% CO2 的环境下温育约16小时。使用9种不同浓度AT9283 (为 1 nM到 10 μM, 对照组为DMSO) 处理细胞,然后再温育72小时。 标记对细胞多倍体形态学的观察。记录产生明显多倍体所需AT9283的浓度。细胞按75−100个细胞/mL接种在有关培养基中,然后转移到6-或24-孔组织培养板上,然后覆盖培养16小时。AT9283(11 种浓度,0.1 nM 到 10 μM) 或对照组(DMSO) 加到复制孔中,DMSO终浓度为0.1%。随后加入AT9283,集落生长10和14天,计算最佳离散菌落数。集落在2 mL Carnoys 固定液(25% 乙酸,75% MeOH)中固定,然后在2 mL 0.4% w/v 结晶紫中染色。计算每孔中集落数。使用Prism Graphpad 软件绘制IC50曲线,通过S形剂量反应曲线计算IC50值。

实验图片 检测方法 检测指标 实验图片 PMID
Growth inhibition assay Cell viability 21430070
体内研究(In Vivo)
体内研究活性

AT9283 按15 mg/kg和 20 mg/kg剂量作用于携带HCT116人结肠癌移植瘤的小鼠,持续16天,显著抑制肿瘤生长,抑制分别达67%和76%。此外, 与血浆(半衰期为0.5小时)相比,AT9283口服给药小鼠,也具有显著较长的半衰期。[1]

动物实验 Animal Models 后腿侧皮下注射HCT116细胞的雄性BALB/c小鼠
Dosages 15 mg/kg 和 20 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01145989 Completed
Multiple Myeloma
NCIC Clinical Trials Group|Astex Pharmaceuticals Inc.|Canadian Cancer Trials Group
February 15 2011 Phase 2
NCT00443976 Completed
Non-Hodgkins Lymphoma|Unspecified Adult Solid Tumor Protocol Specific
NCIC Clinical Trials Group|Astex Pharmaceuticals Inc.|Canadian Cancer Trials Group
January 30 2007 Phase 1

化学信息&溶解度

分子量 381.43 分子式

C19H23N7O2

CAS号 896466-04-9 SDF Download AT9283 SDF
Smiles C1CC1NC(=O)NC2=C(NN=C2)C3=NC4=C(N3)C=C(C=C4)CN5CCOCC5
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 76 mg/mL ( 199.25 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Ethanol : 76 mg/mL

Water : Insoluble

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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