NSC781406

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC₅₀ of 2 nM for PI3Kα. IC50 & Target: IC50: 2 nM (PI3Kα), 1.78 μM (A549 cell), 0.93 μM (HCT116 cells), 1.44 μM (MDA-MB-231 cells), 20 nM (BEL-7404 cells)^[1] In Vitro: NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC₅₀=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC₅₀=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 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 potent against 60 cancer cell lines with a mean GI₅₀ value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines^[1]. In Vivo: In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight^[1].