Barasertib (AZD1152-HQPA)
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥655.00 | 现货 | |
| 1mg | ￥290.00 | 现货 | |
| 2mg | ￥500.00 | 现货 | |
| 5mg | ￥585.00 | 现货 | |
| 10mg | ￥776.00 | 现货 | |
| 25mg | ￥1566.00 | 现货 | |
| 50mg | ￥2583.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
Barasertib（AZD1152-羟基喹唑啉吡唑酰基苯胺（HQPA））是一种有效的Aurora激酶抑制剂。在体内，通过胃肠外给药后，血清中的前体AZD1152被磷酸酶快速裂解，从而产生AZD1152-HQPA。Barasertib对广泛的aurora激酶均有抑制效应，包括aurora A激酶（AKB）、aurora B激酶（ABK）和aurora C激酶（ACK），Ki值分别为1369 nM、0.36 nM和17.0 nM。Barasertib也抑制FMS样酪氨酸激酶3内部串联重复（FLT3-ITD）突变。Barasertib对一系列肿瘤细胞系均具有抗肿瘤活性，包括白血病急性髓细胞白血病（AML）来源的肿瘤细胞。
参考文献：
Martin Grundy, Claire Seedhouse, Nigel H Russell and Monica Pallis. P-glycoprotein and breast cancer resistance protein in acyte myeloid leukaemia cells treated with the aurora-B kinase inhibitor barasertib-Hqpa. BMC Cancer 2011, 11:254
Mike Dennis, Michelle Davies, Stuart Oliver, Roy D’Souza, Laura Pike, and Paul Stockman. Phase I study of the aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia. Cancer Chemother Pharmacol (2012) 70:461-469
产品性质
| 物理外观 | A solid |
| CAS号 | 722544-51-6 |
| 分子式 | C26H30FN7O3 |
| 分子量 | 507.56 |
| 小分子别名 | Barasertib-HQPA |
| 化学名称 | 2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide |
| 溶解度 | ≥25.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| SMILES | CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | Barasertib (AZD1152-HQPA)是一种高选择性的Aurora B抑制剂，IC50值为0.37 nM，比对Aurora A的选择性高约100倍。 |
| 靶点 | Aurora B |
| 生物活性数据 | 0.37 nM |
生物相关数据
质量控制
APExBIO 顾客使用本产品发表的 6 篇科研文献
- 1. Tomoaki Sobajima, Katarzyna M Kowalczyk, et al. "PP6 regulation of Aurora A–TPX2 limits NDC80 phosphorylation and mitotic spindle size." J Cell Biol. 2023 May 1;222(5):e202205117. PMID: 36897279
- 2. Naheed Arfin Borah, Swatishree Sradhanjali, et al. "Aurora Kinase B Expression, Its Regulation and Therapeutic Targeting in Human Retinoblastoma." Invest Ophthalmol Vis Sci. 2021 Mar 1;62(3):16. PMID:33704359
- 3. Maik Schuler, Lindsay Tomlinson, et al. "Experiments in the EpiDerm 3D Skin In Vitro Model and Minipigs In Vivo Indicate Comparatively Lower In Vivo Skin Sensitivity of Topically Applied Aneugenic Compounds." Toxicol Sci. 2021 Feb 26;180(1):103-121. PMID:33481035
- 4. Christine M Field, James F Pelletier, et al. "Disassembly of actin and keratin networks by Aurora B kinase at the midplane of cleaving Xenopus laevis eggs." bioRxiv. 2019 January 06.
- 5. Shodai Tanaka, Kaori Senda-Murata, et al. "Live cell imaging of anaphase bridge formation and the subsequent cleavage furrow regression induced by the Aurora B kinase inhibitor AZD1152-HQPA." Bioimages. 2017.10.05
- 6. Hanley ML, Yoo TY, et al. "Chromosomal passenger complex hydrodynamics suggests chaperoning of the inactive state by nucleoplasmin/nucleophosmin." Mol Biol Cell. 2017 Apr 12. pii: mbc.E16-12-0860. PMID:28404751
沪公网安备 31011002003500