AKT-IN-1 

AKT-IN-1 is an allosteric AKT inhibitor with an IC₅₀ of 1.042 μM.

IC50: 1.042 μM (AKT)^[1]

AKT-IN-1 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

343.42

Solid

C₂₂H₂₁N₃O

1357158-81-6

NC(C1=CN=C(C2=CC=C(C3(N)CCC3)C=C2)C(C4=CC=CC=C4)=C1)=O

Room temperature in continental US; may vary elsewhere.

• [1]. Kettle JG, et al. Diverse heterocyclic scaffolds as allosteric inhibitors of AKT. J Med Chem. 2012 Feb 9;55(3):1261-73.  [Content Brief]