AP26113 |
Dual inhibitor of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR). |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
| Targets | ALK | FER | ROS/ROS1 | FLT3 | FES/FPS | |
| IC50 | 0.62 nM | 1.3 nM | 1.9 nM | 2.1 nM | 3.4 nM |
AP26113 Dilution Calculator
AP26113 Molarity Calculator
| Cas No. | 1197958-12-5 | SDF | Download SDF |
| Chemical Name | 5-chloro-2-N-[4-[4-(dimethylamino)piperidin-1-yl]-2-methoxyphenyl]-4-N-(2-dimethylphosphorylphenyl)pyrimidine-2,4-diamine | ||
| Canonical SMILES | CN(C)C1CCN(CC1)C2=CC(=C(C=C2)NC3=NC=C(C(=N3)NC4=CC=CC=C4P(=O)(C)C)Cl)OC | ||
| Formula | C26H34ClN6O2P | M.Wt | 529.01 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Shipping Condition: | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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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).
References:
[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.
