Limertinib
Limertinib, also known as ASK120067, is an EGFR inhibitor. ASK120067 displayed potent in vitro inhibitory efficacy against Bruton's tyrosine kinase protein and interleukin-2-inducible T cell kinase protein via covalent binding. In cell-based assays, ASK120067 dose-dependently suppressed Bruton's tyrosine kinase phosphorylation and exhibited anti-proliferation potency by inducing apoptosis in numerous B-lymphoma cells. Meanwhile, it caused growth arrest and induced the apoptosis of T-cell leukemia cells by attenuating interleukin-2-inducible T cell kinase activation. Oral administration of ASK120067 led to significant tumor regression in B-cell lymphoma and T-cell leukemia xenograft models by weakening Bruton's tyrosine kinase and interleukin-2-inducible T cell kinase signaling, respectively.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | Limertinib |
|---|---|
| Iupac 化学名称 | N-(5-((5-chloro-4-(naphthalen-2-ylamino)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide |
| 同义词 | ASK120067; ASK 120067; ASK-120067; limertinib, |
| 英文同义词 | ASK120067; ASK 120067; ASK-120067; limertinib, |
| 分子式 | C29H32ClN7O2 |
| 分子量 | 546.06 |
| Smile | CN(CCN(C)C)C1=CC(OC)=C(NC2=NC=C(Cl)C(NC3=CC(C=CC=C4)=C4C=C3)=N2)C=C1NC(C=C)=O |
| InChiKey | QHPVTCLSVVUPOF-UHFFFAOYSA-N |
| InChi | InChI=1S/C29H32ClN7O2/c1-6-27(38)33-23-16-24(26(39-5)17-25(23)37(4)14-13-36(2)3)34-29-31-18-22(30)28(35-29)32-21-12-11-19-9-7-8-10-20(19)15-21/h6-12,15-18H,1,13-14H2,2-5H3,(H,33,38)(H2,31,32,34,35) |
| Cas号 | 1934259-00-3 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 类白色固体 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 0-4℃，可保存几天到几周；-20℃，可保存 几个月。 |
| 可溶性 | 溶于DMSO等有机溶剂 |
| 处理方式 | |
| 运输条件 | 可以在室温下进行运输。 |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Cui X, Wang S, Gao H, Li B, Shi Y, Guo H, Song T, Zheng X. Development of an LC-MS/MS method for quantifying ASK120067, a novel mutant-selective inhibitor of the epidermal growth factor receptor (EGFR) as well as its main metabolite in human plasma and its application in a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2021 Jan 1;1162:122488. doi: 10.1016/j.jchromb.2020.122488. Epub 2020 Dec 7. PMID: 33360679.
2: Zhang T, Qu R, Chan S, Lai M, Tong L, Feng F, Chen H, Song T, Song P, Bai G, Liu Y, Wang Y, Li Y, Su Y, Shen Y, Sun Y, Chen Y, Geng M, Ding K, Ding J, Xie H. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90. doi: 10.1186/s12943-020-01202-9. Erratum in: Mol Cancer. 2021 Aug 17;20(1):102. PMID: 32404161; PMCID: PMC7218543.
