1676893-24-5

NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC₅₀s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively). It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI₅₀ = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.

PI3Kα: 2 nM (IC₅₀); PI3Kγ: 2.7 nM (IC₅₀); PI3Kβ: 9.4 nM (IC₅₀); PI3Kδ: 14 nM (IC₅₀); mTOR: 5.4 nM (IC₅₀)

[1] Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66. DOI:10.1016/j.bmc.2016.01.008