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AP-26113 (brigatinib) is a pan inhibitor of ALK. It is a leading candidate for the treatment of ALK+ non-small-cell lung cancer, especially those with major resistance mechanisms. AP-26113 exhibits efficacy against models of ALK+ anaplastic large cell lymphoma in cases where crizotinib, an approved drug for late-stage and metastatic lung cancers, fails due to developed drug resistance.
| Cas No. | 1197958-12-5 |
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| Purity | ≥98% |
| Formula | C26H34ClN6O2P |
| Formula Wt. | 529.02 |
| IUPAC Name | 5-Chloro-N2-{4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl}-N4-[2-(dimethylphosphoryl)phenyl]-2,4-pyrimidinediamine |
| Synonym | Brigatinib Analog, AP26113 |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Huang W., Liu S., et al. Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase. J Med Chem 59(10):4948-64 (2016). PMID: 27144831.
Ceccon M., Mologni L., et al. Treatment Efficacy and Resistance Mechanisms Using the Second-Generation ALK Inhibitor AP26113 in Human NPM-ALK-Positive Anaplastic Large Cell Lymphoma. Mol Cancer Res. 13(4):775;83 (2015). PMID: 25421750.