AKT-IN-1

SKU: orb1302819

Description

AKT-IN-1

Research Area

Signal Transduction

Key Properties

• CAS Number: 1357158-81-6
• MW: 343.42
• Purity: 98.63%
• Formula: C₂₂H₂₁N₃O
• SMILES: NC(=O)c1cnc(-c2ccc(cc2)C2(N)CCC2)c(c1)-c1ccccc1
• Target: Akt
• Solubility: DMSO:11 mg/mL (32.03 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.82 mM)

Bioactivity

• Target IC50:
  Akt (allosteric):1.04 μM
• In Vivo:
  The effects of AZD-26 in vivo are characterized by measuring the pharmacodynamic activity of AZD-26 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AZD-26 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 AZD-26 is further characterized by measuring the effects on the growth of tumour cell xenografts. Continuous (daily) oral dosing of AZD-26 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumour growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AZD-26 causes significant tumour growth inhibition.
• In Vitro:
  AZD-26 is able to potently inhibit phosphorylation of AKT in cells at both Thr308 (IC50: 0.422 μM) and Ser473 (IC50: 0.322 μM). AZD-26 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AZD-26 potently inhibits the phosphorylation of PRAS40 .

Storage & Handling

• Storage: 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

AKT IN 1, AKTIN1, AKT-IN-1, AZD 26, AZD26, AZD-26, allosteric Akt, Akt, inhibit, Inhibitor, PKB, Protein kinase B

Compound Identifiers

PubChem CID

56953649