- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- qPCR
- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
- 蛋白實(shí)驗(yàn)
- Protein A/G免疫沉淀磁珠
- Anti-DYKDDDDK Tag免疫磁珠
- Anti-DYKDDDDK Tag親和凝膠
- Anti-Myc免疫磁珠
- Anti-HA免疫磁珠
- 磁力架
- Poly DYKDDDDK Tag多肽
- 細(xì)胞核與細(xì)胞漿蛋白抽提試劑盒
- 免疫磁珠
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲液)
- 磷酸酶抑制劑Cocktail
- 細(xì)胞實(shí)驗(yàn)
- Cell Counting Kit-8 (CCK-8)
- 新產(chǎn)品
- 聯(lián)系我們
Barasertib-HQPA (AZD2811)
別名: AZD2811, INH-34, Barasertib-HQPA , Defosbarasertib
Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) 是一種高度選擇性的Aurora B抑制劑，無細(xì)胞試驗(yàn)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-HQPA (AZD2811) Chemical Structure
CAS: 722544-51-6
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
Barasertib-HQPA (AZD2811)相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | Aurora A Aurora B Aurora C Aurora B | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Alisertib (MLN8237) Tozasertib (VX-680) ZM 447439 MLN8054 Danusertib (PHA-739358) Hesperadin MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 PHA-680632 SNS-314 GSK1070916 CCT137690 CYC116 TAK-901 AZD1152(Barasertib) CCT129202 SNS-314 Mesylate LY3295668 SP-96 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復(fù)化合物庫 細(xì)胞周期化合物庫 | 點(diǎn)擊展開 |
相關(guān)信號通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
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(xì)胞試驗(yàn)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(diǎn) |
|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02579226 | Completed | Advanced Solid Tumours |
AstraZeneca |
October 28 2015 | Phase 1 |
|
化學(xué)信息&溶解度
| 分子量 | 507.56 | 分子式 | C26H30FN7O3 |
| CAS號 | 722544-51-6 | SDF | Download Barasertib-HQPA (AZD2811) 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 |
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(jì)算器 |
|
體內(nèi)溶解配方 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(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)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(jì)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(jìn)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 it, cat # S1147, for in vivo use? (IP injection in mice)
回答：
S1147 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.
