KRCA 0008

KRCA 0008 is an inhibitor of anaplastic lymphoma kinase (ALK) and tyrosine non-receptor kinase 2 (TNK2), also known as activated Cdc42 kinase 1 (ACK1; IC₅₀s = 12 and 4 nM, respectively).¹ It is selective for these kinases over the insulin receptor (InsR; IC₅₀ = 210 nM). KRCA 0008 also inhibits the ALK mutants ALK^L1196M, ALK^C1156Y, ALK^F1174L, and ALK^R1275Q (IC₅₀s = 75, 4, 171, and 17 nM, respectively).² It selectively reduces the proliferation of NCI H3122 lung cancer cells, which are driven by the EML4-ALK fusion protein, over NCI H1993 lung cancer cells, which are driven by c-Met (IC₅₀s = 80 and 3,600 nM, respectively). KRCA 0008 (25 and 50 mg/kg) reduces tumor volume in an NCI H3122 mouse xenograft model.

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1. Lee, H.J., Latif, M., Choe, H., et al. K inhibitors of bis-ortho-alkoxy-para-piperazinesubstituted pyrimidines and -triazines for cancer treatment. Arch. Pharm. Res. 37, 1130–1138 (2014).

2. Park, C.H., Choe, H., Jang, I.-Y., et al. Novel bis-ortho-alkoxy-para-piperazinesubstituted-2,4-dianilinopyrimidines (KRCA-0008) as potent and selective ALK inhibitors for anticancer treatment. Bioorg. Med. Chem. Lett. 23(22), 6192-6196 (2013).