AP26113 is an orally-available, potent, and selective inhibitor of ALK with a potency of 0.62 nM against wild-type and activity against a wide range of mutants, including the crizotinib-resistant L1196M line. In a panel of EML4-ALK or NPM-ALK-positive cell lines, AP26113 has IC50 values of 4-31 nM. (1, 2)AP26113 is effective against sensitive and resistant H3122 cells, reducing cell growth, suppressing ALK phosphorylation, and inducing apoptosis. In Ba/F3 cells expressing native or mutant EML4-ALK, AP26113 was active at IC50s of 10 and 24 nM, respectively. (3)
Technical information:
| Chemical Formula: | C26H34ClN6O2P | |
| CAS #: | 1197958-12-5 | |
| Molecular Weight: | 529.01 | |
| Purity: | > 98% | |
| Appearance: | white | |
| Chemical Name: | 2,4-Pyrimidinediamine, 5-chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethylphosphinyl)phenyl]- | |
| Solubility: | Up to 50 mM in DMSO | |
| Synonyms: | AP26113, AP-26113, AP 26113 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Shiao et al., Anaplastic Lymphoma Kinase (ALK) Inhibitors: New Cancer Breakthroughs for Lung Cancer, J. Cancer. Res. Pract. 2011, 27(4), 143-156. |
| 2. | Rivera et al., Efficacy and pharmacodynamic analysis of AP26113, a potent and selective orally active inhibitor of Anaplastic Lymphoma Kinase (ALK). Cancer Res. 2010, 70(8), Suppl 1., AACR 101st Annual Meeting 2010. |
| 3. | Katayama et al., Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK. Proc. Natl. Acad. Sci. 2011, 108(18), 7535-7540. Pubmed ID:21502504 |
Other Information:
Product Specification (pdf) MSDS (pdf) Certificate of Analysis is available upon request.
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