| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| O408946-1ml |
1ml |
现货  |
|
| 别名 | 奥希替尼(AZD9291) |
|---|---|
| 英文别名 | Mereletinib | 2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]- |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Osimertinib (AZD9291) |
| 生化机理 | 奥希替尼 (AZD9291) 是一种口服、不可逆、突变选择性表皮生长因子受体抑制剂，在 LoVo 细胞中对表皮生长因子受体外显子 19 缺失、表皮生长因子受体 L858R/T790M 和表皮生长因子受体 WT 的 IC50 分别为 12.92、11.44 和 493.8 nM。第 3 阶段 |
| 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 | 表皮生长因子受体 erbB1 抑制剂 |
| 产品介绍 |
Osimtinib (AZD9291) 是一种共价结合、不可逆和突变选择性的 EGFR 抑制剂，其有效抑制 L858R (IC50=12 nM) 和 L858R/T790M (IC50=1 nM) EGFR。Osimtinib 解决了肺癌 T790M 突变介导的 EGFR 抑制剂耐药。
Information Osimertinib (AZD9291) is an oral, irreversible, and mutant-selectiveEGFRinhibitor withIC50of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3. AZD9291 shows significantly more potent inhibition of proliferation in mutant EGFR cell lines compared to wild-type in vitro. In vivo AZD9291(5mg/kg p.o.) causes profound regression of tumors across EGFRm+ (PC9) and EGFRm+/T790M (H1975) tumor models with profound inhibition of EGFR phosphorylation and key downstream signaling pathways such as AKT and ERK in vivo. cell lines：HUVECs Concentrations： Incubation Time： Powder Purity:≥99% |
| ALogP | 3.7 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CN1C=C(C2=CC=CC=C21)C3=NC(=NC=C3)NC4=C(C=C(C(=C4)NC(=O)C=C)N(C)CCN(C)C)OC |
| 关联CAS | 1421373-65-0 |
| MeSH Entry Terms | AZD-9291;AZD-9291 mesylate;AZD9291;AZD9291 mesylate;mereletinib;mereletinib mesilate;mereletinib mesylate;N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-2-propenamide;N-(2-((2-(dimethylamino |
| 分子量 | 499.62 |
| Reaxy-Rn | 23334373 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23334373&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 51 mg/mL (198.62 mM); |
|---|
| 象形图 | GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 |
| 1. Xin Zhang, Yuhan Jiang, Na Guo, Yifan Ding, Jingting Feng, Chenyang Miao, Yanni Lv. (2023) Application of SNAP-tag-EGFR cell membrane chromatography model in screening antitumor active components of Silybum marianum (L.) Gaertn. JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (115816). [PMID:37976988] [10.1016/j.jpba.2023.115816] |
| 2. Taotao Huo, Bin Zhu, Xiaoyu Shan, Jiaqi Song, Ziyi Wang, Jianxu Zhou, Xianpeng Zhang, Yuquan Bai, Chengcheng Liu, Yiyang Zhao, Na Mei, Yazhong Bu, Jia Zhang, Guangying Li. (2025) Allicin amplifies disulfidptosis during GOx catalyzing glucose-starvation for cancer therapy via simultaneous antimicrobial and antitumor intervention. CHEMICAL ENGINEERING JOURNAL, 505 (159871). [10.1016/j.cej.2025.159871] |
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