Uses
DC-0068 is a highly selective pan-Akt inhibitor targeting Akt1, Akt2, and Akt3 with IC50 of 5 nM, 18 nM, and 8 nM, respectively.
Uses
GDC-0068 is a highly selective AKT inhibitor targeting Akt1 , Akt2 and Akt3. Studies have shown its use in combination with vemurafenib (V118500), have demonstrated therapeutic value in the treatment of hyperproliferative disorders such as cancer.
Definition
ChEBI: (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]-1-piperazinyl]-3-(propan-2-ylamino)-1-propanone is a N-arylpiperazine.
Biological Activity
gdc-0068 (rg7440) is a highly selective small molecule inhibitor of akt with ic50s of 5, 18 and 8 nm for akt1, akt2 and akt3. 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. gdc-0068 is now used for the treatment of human cancers.1. discovery and preclinical pharmacology of a selective atp-competitive akt inhibitor (gdc-0068) for the treatment of human tumors. jf blake, r xu, jr bencsik, d xiao… - journal of medicinal 20122. lin j, sampath d, nannini ma, et al: targeting activated akt with gdc-0068, a novel selective akt inhibitor that is efficacious in multiple tumor models. clin canc res 2013, 19:1760–1772.
