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Barasertib (AZD1152-HQPA)

別名: AZD2811, INH-34, Barasertib-HQPA , Defosbarasertib 中文名稱：巴拉塞替

Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) 是一種高度選擇性的Aurora B抑制劑，無細胞試驗中IC50為0.37 nM，作用于Aurora B比作用于Aurora A選擇性高3700倍左右。

Barasertib (AZD1152-HQPA) Chemical Structure

Barasertib (AZD1152-HQPA) Chemical Structure

CAS: 722544-51-6

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1375.46 現(xiàn)貨
5mg 976.12 現(xiàn)貨
25mg 3169.53 現(xiàn)貨
200mg 7944.3 現(xiàn)貨
1g 12039.3 現(xiàn)貨
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Barasertib (AZD1152-HQPA)相關(guān)產(chǎn)品

相關(guān)信號通路圖

Aurora Kinase Signaling Pathways

Aurora Kinase信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) 是一種高度選擇性的Aurora B抑制劑，無細胞試驗中IC50為0.37 nM，作用于Aurora B比作用于Aurora A選擇性高3700倍左右。
靶點
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

化學信息&溶解度

分子量 507.56 分子式

C26H30FN7O3
CAS號 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
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (197.02 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 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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