RGNCY-0121 (W934 PI3K/Akt inhibitor)
W934 is a novel PI3/Akt signalling inhibitor which is constantly activated in various cancers. W934 caused an inhibition of PI3Ka kinase in vitro. W349 significantly suppressed the viability of A549 non-small-cell lung cancer cells and HCT116 colorectal cancer cells (IC50 of 0.25 and 0.23 mmol/l respectively). In addition, W934 showed an inhibitory effect on cell migration, invasion and apoptosis. W934 caused an inhibition of G0-G1 phase progression and correspondingly decreased the percentage of cells in S and G2-M phases. W934 was shown to suppress the activation of the PI3K/Akt pathway. Oral administration of W934 in an in vivo A549 xenograft mouse model demonstrated dose dependent tumor inhibition. Thus, W934 has potential as a therapeutic drug candidate for non-small-cell lung cancer.
Systematic Name: (4-((2'-amino-2-morpholino-[4,5'-bipyrimidin]-6-yl)(cyclopropyl)amino)piperidin-1-yl)(3-fluorophenyl)methanone
Mol Wt: 518.60
Tags: Cancer, PI3K, Akt, Tumor, non-small-cell lung carcinoma, colorectal cancer, RGNCY-0121, W934, PI3K/Akt