Akt1 and Akt2-IN-1

SKU: orb1707698

Description

Akt1 and Akt2-IN-1

Research Area

Signal Transduction

Key Properties

• CAS Number: 893422-47-4
• MW: 539.63
• Purity: 99.48%
• Formula: C₃₃H₂₉N₇O
• SMILES: O=c1[nH]ccc2nc(-c3ccc(CN4CCC(CC4)c4n[nH]c(n4)-c4ccccn4)cc3)c(cc12)-c1ccccc1
• Target: Akt
• Solubility: DMSO:35 mg/mL (64.86 mM)

Bioactivity

• Target IC50:
  Akt1:3.5 nM|Akt2:42 nM
• In Vivo:
  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 4.6 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. 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 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.
• In Vitro:
  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. Consistent with the allosteric mode of inhibition, Akt1 and Akt2-IN-1 (Compound 17) is dependent on the PH-domain for Akt inhibition. Akt1 and Akt2-IN-1 (Compound 17) 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).

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Akt2, Akt1 and Akt2 IN 1, Akt1 and Akt2IN1, Akt-1 and Akt2-IN-1, Akt1 and Akt2-IN-1, Akt1

Compound Identifiers

PubChem CID

11656753