Barasertib (AZD1152-HQPA)

别名: AZD2811, INH-34, Barasertib-HQPA , Defosbarasertib 中文名称:巴拉塞替

Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) 是一种高度选择性的Aurora B抑制剂,无细胞试验中IC50为0.37 nM,作用于Aurora B比作用于Aurora A选择性高3700倍左右。

Barasertib (AZD1152-HQPA) Chemical Structure

Barasertib (AZD1152-HQPA) Chemical Structure

CAS: 722544-51-6

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 1375.46 现货
5mg RMB 976.12 现货
25mg RMB 3169.53 现货
200mg RMB 7944.3 现货
1g RMB 12039.3 现货
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客户使用Selleck的Barasertib (AZD1152-HQPA)发表文献145

产品质控

批次: 纯度: 99.98%
99.68

Barasertib (AZD1152-HQPA)相关产品

相关信号通路图

Aurora Kinase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
BT474 Growth Inhibition Assay 0-10000 nM 2-5 d IC50=8 nM 20175926
MDA-MB-231 Growth Inhibition Assay 0-10000 nM 2-5 d IC50=105 nM 20175926
MDA-MB-468 Growth Inhibition Assay 0-10000 nM 2-5 d IC50=14 nM 20175926
MDA-MB-435 Growth Inhibition Assay 0-10000 nM 2-5 d IC50=125 nM 20175926
L450 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
HDLM-2 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
KM-H2 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
L428 Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
Daudi  Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
Raji Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
Ramos Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
BJAJ Apoptosis Assay 500 nM 0-72 h induces apoptosis in a time-dependent manner 21371446
L450 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
HDLM-2 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
KM-H2 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
L428 Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth 21371446
Daudi  Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
Raji Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
Ramos Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
BJAJ Growth Inhibition Assay 500 nM 0-72 h inhibits cell growth significantly 21371446
L540 Function Assay 500 nM 0-72 h inhibits Aurora B kinase 21371446
Daudi  Function Assay 500 nM 0-72 h inhibits Aurora B kinase 21371446
Ramos Function Assay 500 nM 0-72 h inhibits Aurora B kinase 21371446
LNCaP Function Assay 50 nM 48 h induces micronuclei with aneugenic mechanism 25277659
LNCaP Apoptosis Assay 0-500 nM 48 h induces apoptotic cell death through caspase-3 upregulation 25277659
LNCaP Growth Inhibition Assay 0-500 nM 48 h IC50=25 nM 25277659
MDA-MB-361 Growth Inhibition Assay 0-10000 nM 2-5 d IC50=70 nM 20175926
HER18 Growth Inhibition Assay 0-10000 nM 2-5 d IC50=20 nM 20175926
HER18 Apoptosis Assay 100 nM 0/24/48 h induces apoptosis and reduces clonogenic potential 20175926
MDA-MB-231 Apoptosis Assay 105 nM 0/24/48 h induces apoptosis and reduces clonogenic potential 20175926
JHH-1 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=17.4±1.0 nM 19913935
JHH-2 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=218.0±10.8 nM 19913935
JHH-4 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=155.6±16.8 nM 19913935
HuH-1 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=27.3±5.0 nM 19913935
HuH-6 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=3.7±0.6 nM 19913935
HuH-7 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=6.8±0.3 nM 19913935
HLE Growth Inhibition Assay 0.3–1000 nM 72 h EC50=45.9±6.4 nM 19913935
HLF Growth Inhibition Assay 0.3–1000 nM 72 h EC50=126.1±12.2 nM 19913935
PLC/PRF/5 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=76.9±9.9 nM 19913935
SK-Hep1 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=21.9±1.2 nM 19913935
Hep3B Growth Inhibition Assay 0.3–1000 nM 72 h EC50=7.6±1.2 nM 19913935
HepG2 Growth Inhibition Assay 0.3–1000 nM 72 h EC50=14.7±1.7 nM 19913935
Ramos Apoptosis Assay 25/50/100 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
Daudi  Apoptosis Assay 25/50/100 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
BALM-14 Apoptosis Assay 12.5/25/50 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
BALM-27 Apoptosis Assay 12.5/25/50 nM 48 h increases the levels of the cleaved forms of PARP and caspase 3 19823168
NB4 Growth Inhibition Assay 0.01/0.1/1 μM 48 h inhibits cell growth significantly 18367484
HeLa Function Assay 1 uM 24 hrs Inhibition of aurora B autophosphorylation in human HeLa cells at 1 uM after 24 hrs by Western blotting 20684549
HCT116 Growth Inhibition Assay EC50=11±3.3 nM 21245090
SW620 Growth Inhibition Assay EC50=10±2.1 nM 21245090
点击查看更多细胞系数据

生物活性

产品描述 Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) 是一种高度选择性的Aurora B抑制剂,无细胞试验中IC50为0.37 nM,作用于Aurora B比作用于Aurora A选择性高3700倍左右。
靶点
Aurora B [1]
(Cell-free assay)
0.37 nM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02579226 Completed
Advanced Solid Tumours
AstraZeneca
October 28 2015 Phase 1

化学信息&溶解度

分子量 507.56 分子式

C26H30FN7O3

CAS号 722544-51-6 SDF Download Barasertib (AZD1152-HQPA) SDF
Smiles CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 100 mg/mL ( 197.02 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : 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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常见问题及建议解决方法

问题 1:
Can you let me know what solvent I can use for Barasertib, cat # S1147, for in vivo use? (IP injection in mice)

回答:
S1147 Barasertib (AZD1152-HQPA) can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30mg/ml as a clear solution. Usually, when prepare the solution, we will add organic solvents first, then add Tween 80, then water. But this compound can not dissolve in 30% PEG400/0.5% Tween80/5% Propylene glycol clearly. After water was added, it became a clear solution.

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