Barasertib (AZD1152-HQPA)

別名：AZD2811, INH-34, Barasertib-HQPA , Defosbarasertib

製品コード：S1147 純度：99.97%

Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.

CAS No. 722544-51-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 58000	国内在庫あり
50mg	JPY 100500	国内在庫あり
200mg	JPY 145500	国内在庫あり
1g	JPY 220500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（145）

製品安全説明書

現在のバッチを見る：純度： 99.97%

99.97

Barasertib (AZD1152-HQPA)関連製品

関連ターゲット	Aurora A Aurora B Aurora C Aurora B	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library PI3K/Akt Inhibitor Library MAPK Inhibitor Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

Aurora Kinaseシグナル伝達経路

Aurora Kinase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Targets

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

0.37 nM

In Vitro
In vitro	Barasertib (AZD1152-HQPA), a highly selective Aurora B inhibitor, causes polyploidy and apoptosis in many cancer cell lines.^[1]
細胞実験	細胞株	NCI-H82 cells, SCLC and NSCLC cell lines
	濃度	--
	反応時間	--
	実験の流れ	--
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	AURKB / pSer10 Histone H3 / TP53 / CDKN1A / MYCN p53 / p21 / p-p38 / p38		26497213
	Immunofluorescence	p21		24782314
	Growth inhibition assay	Cell viability		26497213

In Vivo
In Vivo	Barasertib (AZD1152-HQPA) is an aurora B kinase inhibitor, and has efficacy against RB1 / SCLC cell line xenografts, RB1 / SCLC PDXs, and autochthonous Rb1 / neuroendocrine tumors.^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02579226	Completed	Advanced Solid Tumours	AstraZeneca	October 28 2015	Phase 1

参考
[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

化学情報

分子量	507.56	化学式	C₂₆H₃₀FN₇O₃
CAS No.	722544-51-6	SDF	Download Barasertib (AZD1152-HQPA) SDFをダウンロードする
Smiles	CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (197.02 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo Batch: Add solvents to the product individually and in order.					投与溶液組成計算機
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	5.0mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.	投与溶液組成計算機
Clear solution	5% DMSO 1 95% corn oil	0.65mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	2.5mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

よくある質問（FAQ）

質問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):