Ipatasertib dihydrochloride (GDC-0068)

Description: Ipatasertib dihydrochloride (formerly also called GDC-0068) is a novel, potent, orally bioavailable, ATP-competitive and highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, it showed 620-fold selectivity over PKA. GDC-0068 is used for the treatment of human cancers. The PI3K-AKT pathway regulates cell growth, survival and tumorigenesis. GDC-0068 binds to and blocks the activation of AKT, which result in cell cycle arrest, inhibition of tumor cell proliferation and induction of tumor cell death. PI3K-AKT is pathway frequently activated in tumors, thus tumors with PTEN or PI3K mutations, which lead to activation of AKT are with high sensitivity to GDC-0068.

References: Clin Cancer Res. 2013 Apr 1; 19(7):1760-72.

Related CAS: 1001264-89-6 (free base); 1489263-16-2 (HCl); 1396257-94-5 (2HCl)