Akt1and Akt2-IN-1 is an allosteric inhibitor ofAkt1(IC₅₀=3.5 nM) andAkt2(IC₅₀=42 nM), with potent and balanced activity.

Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition, is selective for Akt1/2 over Akt3 (IC₅₀=1900 nM), and is highly selective over other members of the AGC family of kinases (>50 μM vs PKA, PKC, SGK). Akt1 and Akt2-IN-1 (Compound 17) has moderate activity in an hERG binding assay (IC₅₀=5610 nM) and is a substrate for human P-glycoprotein^[1].

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) has also been shown to inhibit the growth of A2780 tumors in vivo when used as monotherapy. Akt1 and Akt2-IN-1 (Compound 17) has potent inhibitory activity against Akt1 and 2 in vivo in a mouse lung and efficacy in a tumor xenograft model. Akt1 and Akt2-IN-1 (Compound 17) shows good pharmacokinetics in rat with a low clearance of 4.6 mL/min/kg and a half-life of 3.8 h. 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. Using an acute dosing schedule (IP dosing of 50 mg/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].

539.63

Solid

C₃₃H₂₉N₇O

893422-47-4

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 35 mg/mL(64.86 mM)

*"≥" means soluble, but saturation unknown.

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