计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Barasertib (AZD1152-HQPA), 极光激酶 B 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
AZD1152-HQPA是AZD-1152的活性代谢物，AZD1152-HQPA (Barasertib)是Aurora B 高选择性抑制剂，IC50为0.37 nM，比对Aurora A的抑制性高100倍。A highly selective ARK-2 inhibitor
Information
Barasertib (AZD1152-HQPA, AZD2811, INH-34) is a highly selectiveAurora Binhibitor withIC50of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
In vitro
AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying ~100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM. AZD1152 inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner.
In vivo
Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells. In addition, AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~100 nM
Incubation Time：24 or 48 hours
Powder Purity:≥95%
规格
别名
巴拉塞替尼 (AZD1152-HQPA)
英文别名
AZD2811, INH-34 | 2-(5-(7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-ylamino)-1H-pyrazol-3-yl)-N-(3-fluorophenyl)acetamide
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Barasertib (AZD1152-HQPA)
生化机理
Barasertib（AZD1152-HQPA、AZD2811、INH-34）是一种高选择性极光 B 抑制剂，在无细胞实验中的 IC50 为 0.37 nM，对极光 B 的选择性比对极光 A 的选择性高约 3700 倍。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
极光激酶 B 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
分子量
507.56
Reaxy-Rn
11026336
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11026336&ln=
技术文档
高级数据
关联靶点（人）
FLT3
Tclin
受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3)
(3 活性数据)
MAP4K5
Tchem
丝裂原活化蛋白激酶激酶激酶 5(Mitogen-activated protein kinase kinase kinase kinase 5)
(1 活性数据)
AURKB
Tchem
极光激酶B(Aurora kinase B)
(11 活性数据)
AURKC
Tchem
极光激酶C(Aurora kinase C)
(3 活性数据)
KIT
Tclin
肥大细胞/干细胞生长因子受体试剂盒(Mast/stem cell growth factor receptor Kit)
(7 活性数据)
MAP2K5
Tchem
双特异性丝裂原活化蛋白激酶激酶 5(Dual specificity mitogen-activated protein kinase kinase 5)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 78 mg/mL (181.65 mM); DMSO: 39 mg/mL (90.82 mM); Ethanol: 4 mg/mL (9.31 mM);
折光率
1.68
沸点
796.7° C at 760 mmHg
安全和危险性（GHS）
WGK Germany
3
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 F2414006 |
分析证书 | B408022 |
溶液计算器
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