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  • AP26113
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AP26113

A potent ALK inhibitor

原价
¥875-3812
价格
700-3050
AP26113的二维码

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  • 货号: ajci18808
  • CAS: 1197958-12-5
  • 别名: Brigatinib analog
  • 分子式: C26H34ClN6O2P
  • 分子量: 529.01
  • 纯度: >98%
  • 溶解度: ≥ 26.45mg/mL in DMSO
  • 储存: Store at -20°C
  • 库存: 现货

Background

AP26113 is a novel, synthetic, orally available small-molecule inhibitor of anaplastic lymphoma kinase (ALK), which is a receptor tyrosine kinase in the insulin receptor superfamily, with half maximal inhibitory concentration IC50 ranging from 5 nmol/l to 11 nmol/l. AP26113 is also capable of inhibiting the ALK tyrosine kinase gatekeeper mutation L1196M (IC50: 15 nmol/l to 45 nmol/L), mutant epidermal growth factor receptor (EGFR) containing the gatekeeper T790M mutation and c-ros oncogene 1 (ROS1). Moreover, AP26113 has been found to be active against H3122 cells (both sensitive and resistant) and Ba/F3 cells harboring native or mutant EML4-ALK (IC50: 10 nM and 24 nM respectively).

参考文献:
[1]Solomon B, Wilner KD, Shaw AT. Current status of targeted therapy for anaplastic lymphoma kinase-rearranged non-small cell lung cancer. Clin Pharmacol Ther. 2014 Jan;95(1):15-23. doi: 10.1038/clpt.2013.200. Epub 2013 Oct 3.
[2]Katayama R1, Khan TM, Benes C, Lifshits E, Ebi H, Rivera VM, Shakespeare WC, Iafrate AJ, Engelman JA, Shaw AT. Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc Natl Acad Sci U S A. 2011 May 3;108(18):7535-40. doi: 10.1073/pnas.1019559108. Epub 2011 Apr 18.

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