Description
CCT128930 is a novel ATP-competitive AKT2 inhibitor with IC50 of 6 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C18H20ClN5
Chemical Name
4-(4-chlorobenzyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine
Solubility
DSMO 68 mg/mL Water
In vitro
CCT128930 is a novel ATP-competitive AKT2 inhibitor with IC50 of 6 nM. CCT128930 is a high selective inhibitor with a 28-fold selectivity over the closely related PKA kinase. CCT128930 inhibit PKA and p70S6K with IC50 of 168 nM and 120 nM. CCT128930 inhibit the growth of U87MG human glioblastoma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells with IC50 of 6.3 umol/L, 0.35 umol/L and 1.9 umol/L. CCT128930 can influence cell cycle by inhibiting akt. CCT128930 cause a predominant G1-phase arrest, with a corresponding decrease in S phase in PTEN-null U87MG human glioblastoma cells in a time- and drug concentration-dependent manner.
In vivo
In PTEN-null U87MG human glioblastoma xenografts and HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, CCT128930 (25 mg/kg, 40 mg/kg) shows antitumor activity as a single agent.
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