In vitro activity: AS 602801 (AS602801) treatment induces cell death and accordingly decreased the number of viable cells in all three cell lines in a dose-dependent manner, suggesting that AS 602801 may have selective cytotoxic activity against neoplastic cells. AS 602801 exhibits cytotoxicity against both serum-cultured non-stem cancer cells and cancer stem cells derived from human pancreatic cancer, non-small cell lung cancer, ovarian cancer and glioblastoma at concentrations that did not decrease the viability of normal human fibroblasts. AS 602801 also inhibits the self-renewal and tumor-initiating capacity of cancer stem cells surviving AS 602801 treatment.

Kinase Assay: AS602801 (also known as Bentamapimod and PGL5001) is a novel, potent and ATP-competitive JNK (c-Jun N-terminal Kinase) inhibitor with IC50 values of 80 nM, 90 nM, and 230 nM for JNK1, JNK2, and JNK3, respectively. It acts as a JNK inhibitor which could reduce the surface and volume of induced endometriosis in the baboon without any significant effect on cycle length or serum reproductive hormones, and without significant endocrine side effects.

Cell Assay: PANC-1, A2780, and A549 human cancer cells and IMR90 human normal fibroblasts are treated without (control) or with the indicated concentrations of AS 602801 (2.5, 5, and 7.5 μM) for 3 days. The number of viable cells (left panels) and the percentage of dead cells (right panels) are determined using trypan blue as a vital dye.