1357158-81-6

1357158-81-6 structure

Name	6-(4-(1-aminocyclobutyl)phenyl)-5-phenylnicotinamide
Synonyms	6-[4-(1-Aminocyclobutyl)phenyl]-5-phenylnicotinamide 3-Pyridinecarboxamide, 6-[4-(1-aminocyclobutyl)phenyl]-5-phenyl- 6-[4-(1-Aminocyclobutyl)phenyl]-5-phenyl-3-pyridinecarboxamide AZD-26 AKT-IN-1

Description	AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.
Related Catalog	Signaling Pathways >> PI3K/Akt/mTOR >> Akt Research Areas >> Cancer
Target	IC50: 1.042 μM (AKT)[1]
In Vitro	AKT-IN-1 (Compound 26) is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC50s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40[1].
In Vivo	The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition[1].
References	[1]. Kettle JG, et al. Diverse heterocyclic scaffolds as allosteric inhibitors of AKT. J Med Chem. 2012 Feb 9;55(3):1261-73.