| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B408022-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 极光激酶 B 抑制剂 |
| 产品介绍 |
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. 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 lines： Concentrations：Dissolved in DMSO, final concentrations ~100 nM Incubation Time：24 or 48 hours Powder Purity:≥95% |
| 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= |
| 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 |
| WGK Germany | 3 |
|---|
首页
400-620-6333
