Based on the unique expression of LAT1 on both the BBB and tumor cells and the potent anti-tumor activity of the tertiary bis(2-chloroethyl)amine class of chemotherapeutics, we have discovered a novel chemical entity (QBS10072S), which combines the molecular characteristics of a selective LAT1 substrate with the validated therapeutic properties of tertiary bis(2-chloroethyl)amine drugs. The gene discussed is SLC7A5; the disease is neoplasm.