NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 2 nM for PI3Kα).

NSC781406 shows reasonable liver microsome stability. NSC781406 displays effective PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM) and it also demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is effective against 60 cancer cell lines with a mean GI50 value of 65 nM and with a GI50 value of less than 10 nM against four cancer cell lines.

NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight. NSC781406(30 mg/kg) treatment, causes statistically significant antitumor activity, in the xenograft models. It has a mean reduction in the relative tumor volume ratio of 52%. Sorafenib shows an inhibition ratio of 44% at 50 mg/kg .