In this paper, we describe the cytotoxic potency of LASSBio-2208 (4) in different tumour cells lines, its antiproliferative profile, the study of pharmacological synergism between LASSBio-2208 (4) with gedatolisib (PI3K and mTOR inhibitor), tubastatin A (HDAC-6 inhibitor), or LASSBio-1911 (3) (HDAC-6/8 inhibitor), and the attempts to determine its in vitro drug metabolism and pharmacokinetics (DMPK) profile. This evidence concerns the gene PIK3CA and neoplasm.