Barasertib (AZD1152-HQPA)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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
- 1. 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
- 2. 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
- 3. 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.
- 4. 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
- 5. 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
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 507.56 |
| Cas No. | 722544-51-6 |
| Formula | C26H30FN7O3 |
| Synonyms | AZD1152-HQPA,AZD-1152HQPA, AZD1152 HPQA,INH 34 |
| Solubility | ≥25.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| Chemical Name | 2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide |
| SDF | Download SDF |
| Canonical SMILES | CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验 [1]: | |
|
细胞系 |
HL-60细胞 |
|
制备方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液，一般步骤如下：请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
|
反应条件 |
25 nM，72 hours |
|
实验结果 |
在Barasertib处理的24-48小时内，细胞4N和8N的DNA含量增加，意味着产生了多倍体。48-72小时后，与未处理的细胞相比，barasertib-HQPA通过增加亚G1群体数量，诱导凋亡性细胞死亡。 在24-48小时明显诱导多倍体产生，此后，细胞核显示出典型的凋亡形态，例如核碎裂和固缩。这些观察结果符合流式细胞术分析的结果。 |
| 动物实验[2]: | |
|
动物模型 |
注射SW620、Colo205或HCT116细胞的雌性裸鼠 |
|
给药剂量 |
皮下注射，150 mg/kg/day，48小时微量泵输注 |
|
实验结果 |
在SW620、HCT116和Colo205异种移植肿瘤中分别观察到79％（P < 0.001，第23天）、60％（P < 0.001，第25天）和81％（P < 0.05，第21天）的肿瘤生长抑制。Colo205异种移植物对barasertib治疗最敏感，在细胞移植后21天平均肿瘤体积（±SEM）为0.42 ± 0.19 cm3，而对照动物为2.24 ± 0.75 cm3（P < 0.05）。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Yamauchi T, Uzui K, Shigemi H, et al. Aurora B inhibitor barasertib and cytarabine exert a greater-than-additive cytotoxicity in acute myeloid leukemia cells. Cancer science, 2013, 104(7): 926-933. [2] Alferez D G, Goodlad R A, Odedra R, et al. Inhibition of Aurora-B kinase activity confers antitumor efficacy in preclinical mouse models of early and advanced gastrointestinal neoplasia. International journal of oncology, 2012, 41(4): 1475-1485. |
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| 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 | |||||
| IC50 | 0.37 nM | |||||
质量控制和MSDS
- 批次：
化学结构
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