Akt1 and Akt2-IN-1, Inhibitor | Akt1, inhibitor

Akt1 and Akt2-IN-1

Cat. Num. AAA5754492

• Purity: 98.00%
• Synonyms: Akt1 and Akt2-IN-1; Akt1; inhibitor

• Purity/Purification: 98.00%
• Form/Format: Solid. Powder

• Solubility: DMSO: 35mg/mL (64.86mM); (<1mg/ml refers to the product slightly soluble or insoluble)
• Formula: C33H29N7O
• SMILES: 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
• CAS Number: 893422-47-4
• Target & IC50: Akt1: ic50 3.5nM; Akt2: ic50 42nM
• In Vitro: 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].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Akt1, inhibitor

Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50=3.5nM) and Akt2 (IC50=42nM). It has potent and balanced activity.

Product Categories/Family for Akt1, inhibitor

Cytoskeletal Signaling; Akt; PI3K/Akt/mTOR signaling

References

Bilodeau MT, Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3178-82.
Bilodeau MT, Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3178-82.