ASP3026

ASP3026 is an inhibitor of anaplastic lymphoma kinase (ALK; IC₅₀s = 3.5, 10, and 5.4 nM for the wild-type, ALK^F1174L, and ALK^R1275Q enzymes, respectively).¹ It is selective for ALK over a panel of 86 kinases at 1,000 nM but also inhibits c-Ros oncogene 1 (ROS1) and tyrosine kinase non-receptor 2 (TNK2; IC₅₀s = 8.9 and 5.8 nM, respectively). ASP3026 inhibits the proliferation of Ba/F3 cells expressing nucleophosmin (NPM) or echinoderm microtubule-associated protein-like 4 (ELM4) ALK fusion proteins (IC₅₀s = 84 and 56 nM for NPM-ALK and ELM4-ALK, respectively), as well as several Ba/F3 cells expressing NPM-ALK or ELM4-ALK mutants that are resistant to the c-Met and ALK inhibitor crizotinib (Item No. 12087).² It induces tumor regression in an NCI H2228 non-small cell lung cancer (NSCLC) mouse xenograft model when administered at doses of 10 and 30 mg/kg.¹

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1. Mori, M., Ueno, Y., Konagai, S., et al. The selective anaplastic lymphoma receptor tyrosine kinase inhibitor ASP3026 induces tumor regression and prolongs survival in non-small cell lung cancer model mice. Mol. Cancer Ther. 13(2), 329-340 (2015).

2. Fontana, D., Ceccon, M., Gambacorti-Passerini, C., et al. Activity of second-generation ALK inhibitors against crizotinib-resistant mutants in an NPM-ALK model compared to EML4-ALK. Cancer Med. 4(7), 953-965 (2016).