RGNCY-0121 (W934 PI3K/Akt inhibitor)

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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

SMILES:  NC(N=C1)=NC=C1C2=CC(N(C3CC3)C4CCN(C(C5=CC=CC(F)=C5)=O)CC4)=

NC(N6CCOCC6)=N2

Formula:   C27H31FN8O2

Mol Wt: 518.60