AZD-9291 mesylate
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.
第一代EGFR酪氨酸激酶抑制剂(EGFR TKI)为晚期EGFR突变(EGFRm)的非小细胞肺癌(NSCLC)患者提供了显著的临床效益.NSCLC患者病情恶化通常是由耐药突变引起的.AZD9291是一种可口服的\有效的和选择性的第三代EGFRm敏感突变体和T790M耐药突变体的不可逆抑制剂,对野生型EGFR无效.
体外实验:在EGFRm和EGFRm/T790M突变的细胞系中,AZD9291有效抑制信号通路和细胞生长,对野生型EGFR细胞系具有更低的活性.AZD9291对L858R和L858R/T790M EGFRm的IC50值分别为12 nmol/L和1 nmol/L[1].
体内实验:AZD9291具有良好的生物利用度,广泛分布于组织中.在口服给药的小鼠中,AZD9291具有中等的清除率,其半衰期约为3小时.在PC-9(ex19del)和H1975(L858R/T790M)肿瘤异种移植模型中,给予AZD9291,每天一次,显著引起剂量依赖性肿瘤消退.在低至2.5 mg kg-1(每天一次)的剂量下,可以观察到两个模型中的肿瘤缩小[1].
临床试验:目前,AZD9291的甲磺酸盐正处于剂量递增I期临床试验(AURA;NCT01802632;AstraZeneca)阶段,用于治疗接受了各种EGFR TKI治疗(包括Gefitinib或Erlotinib)但病情仍然恶化的晚期EGFRm NSCLC患者.I期临床试验表明,AZD9291在首次剂量下已显示出良好的疗效.
参考文献：
[1] Cross DA, Ashton SE, Ghiorghiu S, Eberlein C, Nebhan CA, Spitzler PJ, Orme JP, Finlay MR, Ward RA, Mellor MJ, Hughes G, Rahi A, Jacobs VN, Red Brewer M, Ichihara E, Sun J, Jin H, Ballard P, Al-Kadhimi K, Rowlinson R, Klinowska T, Richmond GH, Cantarini M, Kim DW, Ranson MR, Pao W. AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014;4(9):1046-61.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 595.71 |
| Cas No. | 1421373-66-1 |
| Formula | C29H37N7O5S |
| Solubility | insoluble in EtOH; insoluble in DMSO; insoluble in H2O |
| Chemical Name | (Z)-N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylimidic acid compound with methanesulfonic acid (1:1) |
| SDF | Download SDF |
| Canonical SMILES | C=C/C(O)=N/C1=CC(NC2=NC=CC(C(C3=CC=CC=C34)=CN4C)=N2)=C(OC)C=C1N(CCN(C)C)C.CS(O)(=O)=O |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
