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Barasertib {[allProObj[0].p_purity_real_show]}

货号：A363646 同义名： Azd1152 Ambeed 开学季，买赠积分，赢豪礼

Barasertib (AZD1152) 是 Barasertib-hQPA 的前药，是一种高选择性的 Aurora B 抑制剂，IC50 为 0.37 nM。Barasertib (AZD1152) 可诱导癌细胞生长停滞和凋亡。

Barasertib 化学结构 CAS号：722543-31-9
Barasertib 化学结构
CAS号：722543-31-9
Barasertib 3D分子结构
CAS号：722543-31-9
Barasertib 化学结构 CAS号：722543-31-9
Barasertib 3D分子结构 CAS号：722543-31-9
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Barasertib 纯度/质量文件 产品仅供科研

货号：A363646 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Aurora A ↓ Aurora B ↓ Aurora C ↓ 其他靶点 纯度
BI-847325 ++

Aurora A (Human), IC50: 25 nM

 		++++

Aurora B (Xenopus laevis), IC50: 3 nM

 		++

Aurora C (Human), IC50: 15 nM

 		{[allProObj[0].p_purity_real_show]}
CCT 137690 ++

Aurora A, IC50: 15 nM

 		++

Aurora B, IC50: 25 nM

 		++

Aurora C, IC50: 19 nM

 		{[allProObj[0].p_purity_real_show]}
MK-5108 ++++

Aurora A, IC50: 0.064 nM

 		{[allProObj[0].p_purity_real_show]}
KW-2449 +

Aurora A, IC50: 48 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
Tozasertib ++++

Aurora A, Ki app: 0.6 nM

 		++

Aurora B, Ki app: 18 nM

 		+++

Aurora C, Ki app: 4.6 nM

 		FLT3,Bcr-Abl {[allProObj[0].p_purity_real_show]}
AT9283 ++++

Aurora A, IC50: ~3.0 nM

 		++++

Aurora B, IC50: ~3.0 nM

 		{[allProObj[0].p_purity_real_show]}
MLN8054 +++

Aurora A, IC50: 4 nM

 		+

Aurora B, IC50: 172 nM

 		{[allProObj[0].p_purity_real_show]}
ZM-447439 +

Aurora A, IC50: 110 nM

 		+

Aurora B, IC50: 130 nM

 		Src {[allProObj[0].p_purity_real_show]}
TCS7010 ++++

Aurora A, IC50: 3.4 nM

 		{[allProObj[0].p_purity_real_show]}
TAK-901 ++

Aurora A-TPX2, IC50: 21 nM

 		++

Aurora B-INCENP, IC50: 15 nM

 		{[allProObj[0].p_purity_real_show]}
Danusertib +++

Aurora A, IC50: 13 nM

 		+

Aurora B, IC50: 79 nM

 		+

Aurora C, IC50: 61 nM

 		RET {[allProObj[0].p_purity_real_show]}
MK-8745 ++++

Aurora A, IC50: 0.6 nM

 		{[allProObj[0].p_purity_real_show]}
PHA-680632 ++

Aurora A, IC50: 27 nM

 		+

Aurora B, IC50: 135 nM

 		+

Aurora C, IC50: 120 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
AMG 900 +++

Aurora A, IC50: 5 nM

 		+++

Aurora B, IC50: 4 nM

 		++++

Aurora C, IC50: 1 nM

 		{[allProObj[0].p_purity_real_show]}
Alisertib ++++

Aurora A, IC50: 1.2 nM

 		{[allProObj[0].p_purity_real_show]}
ENMD-2076 +++

Aurora A, IC50: 14 nM

 		+

Aurora B, IC50: 350 nM

 		FLT3,RET {[allProObj[0].p_purity_real_show]}
JNJ-7706621 +++

Aurora A, IC50: 11 nM

 		++

Aurora B, IC50: 15 nM

 		{[allProObj[0].p_purity_real_show]}
CYC-116 +++

Aurora A, Ki: 8 nM

 		+++

Aurora B, Ki: 9 nM

 		FLT3 {[allProObj[0].p_purity_real_show]}
Reversine +++

Aurora A, IC50: 12 nM

 		+++

Aurora B, IC50: 13 nM

 		++

Aurora C, IC50: 20 nM

 		{[allProObj[0].p_purity_real_show]}
CCT129202 ++

Aurora A, IC50: 42 nM

 		+

Aurora B, IC50: 198 nM

 		+

Aurora C, IC50: 227 nM

 		{[allProObj[0].p_purity_real_show]}
SNS-314 mesylate +++

Aurora A, IC50: 9 nM

 		++

Aurora B, IC50: 31 nM

 		++++

Aurora C, IC50: 3 nM

 		{[allProObj[0].p_purity_real_show]}
Barasertib-HQPA ++++

Aurora B, IC50: 0.37 nM

 		{[allProObj[0].p_purity_real_show]}
Hesperadin +

Aurora B (human), IC50: 250 nM

 		{[allProObj[0].p_purity_real_show]}
GSK-1070916 ++++

Aurora B-INCENP, IC50: 3.5 nM

 		+++

Aurora C-INCENP, IC50: 6.5 nM

 		SIK,Tie-2 {[allProObj[0].p_purity_real_show]}
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Barasertib 生物活性

描述 Barasertib, also known as AZD1152, is the precursor to Barasertib-hQPA and is a potent inhibitor of Aurora B kinase, demonstrating an IC50 value of 0.37 nM in cell-free assays. It is known to halt cell proliferation and promote apoptosis in various cancer cells. When applied to freshly isolated leukemia cells at a concentration of 3 μM for 3 hours, Barasertib-HQPA markedly reduces the levels of phosphorylated histone H3[1]. Barasertib-hydroxyquinazoline pyrazol anilide (HQPA) is swiftly transformed into the active form, Barasertib-HQPA, within the plasma[2]. Barasertib-HQPA elicits a significant anti-proliferative response, resulting in the emergence of a polyploid cell population, often culminating in apoptosis[3].

Barasertib 动物研究

Animal study Barasertib at a dosage of 25 mg/kg, significantly reduces the growth and mass of tumors treated with AZD1152. Furthermore, Barasertib at 5 mg/kg improves the efficacy of vincristine or daunorubicin in curbing the growth of human MOLM13 leukemic xenografts[1]. When administered at doses ranging from 10 to 150 mg/kg/day, Barasertib effectively hampers the growth of xenografts of human colon, lung, and blood tumors in immunodeficient mice. The average inhibition of tumor growth observed was between 55% to 100%[2].

Barasertib 参考文献

[1]Yang J, et al. AZD1152, a novel and selective aurora B kinase inhibitor, induces growth arrest, apoptosis, and sensitization for tubulin depolymerizing agent or topoisomerase II inhibitor in human acute leukemia cells in vitro and in vivo. Blood. 2007 Sep

[2]Oke A, et al. AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo. Cancer Res. 2009 May 15;69(10):4150-8.

[3]Wilkinson RW, et al. AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res. 2007 Jun 15;13(12):3682-8.

Barasertib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.51mL

1.70mL

0.85mL

17.02mL

3.40mL

1.70mL

Barasertib 技术信息

CAS号722543-31-9
分子式C26H31FN7O6P
分子量 587.54
别名 Azd1152
运输蓝冰
存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度

DMSO: 35 mg/mL(59.57 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Barasertib | 722543-31-9 | AZD1152 | AZD 1152 | AZD-1152 | Aurora B Inhibitor | Cell Cycle/DNA Damage | Epigenetics | Apoptosis | Aurora Kinase | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Barasertib 纯度/质量文件 | Barasertib 亚型比较 | Barasertib 生物活性 | Barasertib 参考文献 | Barasertib 实验方案 | Barasertib 技术信息

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