A derivative of erlotinib
TD52 is a derivative of the EGFR tyrosine kinase inhibitor erlotinib .1 It decreases the viability of HA22T, Hep3B, PLC/PRF/5, and SK-HEP-1 hepatocellular carcinoma cells (IC50s = 0.9, 0.9, 0.8, and 1.2 ?M, respectively). TD52 induces apoptosis in a variety of cancer cells, including HA22T and Hep3B hepatocellular carcinoma and HCC1937 and MDA-MB-231 triple-negative breast cancer cells in a concentration-dependent manner.1,2 TD52 (10 mg/kg per day) increases intratumoral protein phosphatase 2A (PP2A) activity, reduces intratumoral cancerous inhibitor of PP2A (CIP2A) and phosphorylated Akt levels, and reduces tumor growth in a PLC/PRF/5 mouse xenograft model.1
1.Yu, H.-C., Hung, M.-H., Chen, Y.-L., et al.Erlotinib derivative inhibits hepatocellular carcinoma by targeting CIP2A to reactivate protein phosphatase 2ACell Death Dis.5(7)e1359(2014) 2.Liu, C.-Y., Huang, T.-T., Huang, C.-T., et al.EGFR-independent Elk1/CIP2A signalling mediates apoptotic effect of an erlotinib derivative TD52 in triple-negative breast cancer cellsEur. J. Cancer72112-123(2017)
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