AKT1 Inhibitor – and Akt2-in-1

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

539.63

DMSO: 35mg/mL (64.86mM)
(<1mg/ml refers to the product slightly soluble or insoluble)

C33H29N7O

O=C(NC=C1)C2=C1N=C(C(C3=CC=CC=C3)=C2)C(C=C4)=CC=C4CN5CCC(CC5)C6=NNC(C7=NC=CC=C7)=N6

893422-47-4

Akt1: ic50 3.5nM
Akt2: ic50 42nM

Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in at exposures that provide high levels of Akt1 and 2 inhibition in vivo. Akt1 and Akt2-IN-1 (Compound 17) shows good pharmacokinetics in rat with a low clearance of 4.6mL/min/kg and a half-life of 3.8 hours. Due to the improved cell potency, physical properties, and rodent pharmacokinetics of Akt1 and Akt2-IN-1 (Compound 17), tolerability and Akt inhibition are assessed in mice. Akt1 and Akt2-IN-1 (Compound 17) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy and has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Using an acute dosing schedule (IP dosing of 50mg/kg at times 0, 3, and 8 h), administration of Akt1 and Akt2-IN-1 (Compound 17) is well tolerated in mice and shows high levels of Akt inhibition in mouse lung[1].

Cytoskeletal Signaling; Akt; PI3K/Akt/mTOR signaling