AZD8330
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.
AZD8330是一种口服有效的MEK1/2的选择性抑制剂，IC50值为7 nM。AZD8330通过抑制MEK1/2，抑制生长因子介导的细胞信号传导和肿瘤细胞增殖。
MEK又称为MAP激酶激酶（MAP2K），是一种激酶，参与磷酸化促分裂原活化蛋白激酶（MAPK）。MAPK信号通路的活化参与各种细胞过程的调控，包括细胞增殖、分化、凋亡、代谢和炎症。
在 Burkitt's淋巴瘤细胞系Raji细胞中，AZD8330以时间和剂量依赖的方式抑制ERK1/2信号转导途径的活化，导致细胞凋亡[1]。
在82例晚期恶性肿瘤中进行I期临床试验，定义了AZD8330的最大耐受剂量（MTD），并评估了安全性、耐受性、药代动力学和药效。该物质的MTD为40 mg/day [2]。
参考文献：
1. Feng K, Wang C, Zhou H, Yang J, Dong L, Zhou K, et al. [Effect of ERK1/2 inhibitor AZD8330 on human Burkitt's lymphoma cell line Raji cells and its mechanism]. Zhonghua Xue Ye Xue Za Zhi 2015,36:148-152.
2. Cohen RB, Aamdal S, Nyakas M, Cavallin M, Green D, Learoyd M, et al. A phase I dose-finding, safety and tolerability study of AZD8330 in patients with advanced malignancies. Eur J Cancer 2013,49:1521-1529.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 461.23 |
| Cas No. | 869357-68-6 |
| Formula | C16H17FIN3O4 |
| Synonyms | ARRY-424704; ARRY-704; AZD-8330; ARRY424704; ARRY704; AZD8330 |
| Solubility | ≥23.05 mg/mL in DMSO; insoluble in H2O; ≥46.1 mg/mL in EtOH |
| Chemical Name | 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxopyridine-3-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=CC(=C(N(C1=O)C)NC2=C(C=C(C=C2)I)F)C(=O)NOCCO |
| 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]: | |
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细胞系 |
MOS、U2OS、KPD、ZK58、143b和Saos-2细胞 |
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制备方法 |
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 °C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 °C可放置数月。 |
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反应条件 |
0 ~ 1 μM；72小时 |
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实验结果 |
AZD8330降低MOS和U2OS细胞的活力，同时显著影响143b细胞。相比之下，AZD8330对KPD、ZK58和Saos-2细胞的活力没有影响。capase3/7活性测定结果表明，0.5μM AZD8330诱导MOS和U2OS细胞凋亡，但不能诱导KPD和ZK58细胞凋亡。 |
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References: [1]. Zuzanna Baranski, Tijmen H. Booij, Marieke L. Kuijjer, Yvonne de Jong, Anne-Marie Cleton-Jansen, Leo S. Price, Bob van de Water, Judith V. M. G. Bovée, Pancras C.W. Hogendoorn, Erik H.J. Danen. MEK inhibition induces apoptosis in osteosarcoma cells with constitutive ERK1/2 phosphorylation. Genes Cancer. 2015 Nov; 6(11-12): 503–512. |
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| Description | AZD8330是一种新型的、选择性的和非ATP竞争性的MEK1/2抑制剂，IC50值为7 nM。 | |||||
| 靶点 | ERK phosphorylation | MEK1/2 | ||||
| IC50 | 0.4 nM | 7 nM | ||||
质量控制和MSDS
- 批次:
化学结构
