Description: Ipatasertib (GDC-0068) (GDC-0068), a highly specific pan-Akt inhibitor, targets Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, respectively. Target: Akt. Smiles: C[C@H]1C2=C(N=CN=C2[C@H](O)C1)N3CCN(C([C@H](CNC(C)C)C4=CC=C(Cl)C=C4)=O)CC3. References: Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01.

GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays. It is 620-fold selective for Akt over protein kinase A and has been shown to block Akt signaling selectively in cultured tumor cell lines characterized by...

GDC-0068 is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (PKB, protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway.