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| 品牌 | absin | CAS | 1374640-70-6 |
|---|---|---|---|
| 分子式 | C27H28F3N7O3 | 纯度 | ＞98% |
| 分子量 | 555.55 | 货号 | abs810462 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a novel, irreversible and orally deli | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
CO1686 1374640-70-6
| 产品描述 | |
| 描述 | CO-1686 is a novel, irreversible and orally delivered kinase inhibitor that specifically targets the mutant forms of EGFR including T790M(IC50=21 nM). |
| 纯度 | >98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | Rociletinib, AVL-301; CNX-419,co 1686,co1686 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO 100 mg/mL (180.0 mM) |
| 生物活性 | |
| 靶点 | EGFR (L858R/T790M) ,EGFR (wt) |
| In vitro(体外研究) | CO-1686 inhibits p-EGFR with IC50 ranging from 62 to 187 nM in the mutant EGFR–expressing cells, while inhibits EGFR phosphorylation with IC50 of > 2,000 nM in the three WT EGFR–expressing cells. CO-1686 selectively inhibits growth of NSCLC cells expressing mutant EGFR with GI50 ranging from 7 to 32 nM, and induces apoptosis. CO-1686–resistant NSCLC cell lines exhibits signs of epithelial-mesenchymal transition and increased sensitivity to AKT inhibitors. |
| In vivo(体内研究) | CO-1686 causes dose-dependent and significant tumor growth inhibition in all EGFR-mutant models as well as human EGFRL858R- and EGFRL858R/T790M-expressing transgenic mice. |
| 研究领域 | |
| 研究领域 | CancerGrowth factorsEGF CancerOncoproteins/suppressorsOncoproteinsGrowth factor receptors CancerSignal transductionProtein phosphorylationTyrosine kinasesReceptor tyrosine kinases CancerTumor biomarkersReceptors Cell CycleCell differentiation MicrobiologyOrganismVirusDNA VirusssRNA positive strand virusSARS Coronavirus NeuroscienceDevelopment NeuroscienceProcesses Signal TransductionGrowth Factors/HormonesEGF Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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