Barasertib (AZD1152-HQPA)

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

目录号：S1147 Purity: 99.98%

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

CAS: 722544-51-6

规格	价格	库存
10mM (1mL in DMSO)	1375.46	现货
5mg	976.12	现货
25mg	3169.53	现货
200mg	7944.3	现货
1g	12039.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次：纯度： 99.98%

99.98

Barasertib (AZD1152-HQPA)相关产品

相关靶点	Aurora A Aurora B Aurora C Aurora B	点击展开
相关产品	Alisertib (MLN8237) Tozasertib (VX-680) ZM 447439 MLN8054 Hesperadin Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 PHA-680632 SNS-314 CCT137690 GSK1070916 CYC116 TAK-901 CCT129202 SNS-314 Mesylate LY3295668 SP-96	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 DNA损伤/ DNA修复化合物库细胞周期化合物库	点击展开

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

靶点

Aurora B ^[1]
(Cell-free assay)

0.37 nM

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT02579226	Completed	Advanced Solid Tumours	AstraZeneca	October 28 2015	Phase 1

参考文献
[1] Oser, Matthew G et al. Cancer discovery vol. 9,2 (2019): 230-247. [2] Yang J, et al. Blood. 2007 Sep 15;110(6):2034-40.

参考文献

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)	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 : 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

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

DMSO : 102 mg/mL ( (200.96 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 3 mg/mL (5.91 mM)

Water : Insoluble

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

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
=	×	×

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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操作手册

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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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Barasertib (AZD1152-HQPA)

产品质控

Barasertib (AZD1152-HQPA)相关产品

相关信号通路图

细胞实验数据示例

生物活性

化学信息&溶解度

实验计算

技术支持

常见问题及建议解决方法