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Biological Description

Description: Afuresertib is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

Targets&IC50: Akt3:2.6 nM(Ki), Akt2:2 nM(Ki), Akt1:0.08 nM(Ki)

Kinase Assay: Potency (Ki*) of afuresertib: The true potency (Ki*) of the inhibitor is initially determined at low enzyme concentrations (0.1 nM AKT1, 0.7 nM AKT2, and 0.2 nM AKT3) using a filter binding assay and then confirmed with progress curve analysis. In the filter binding assay, a pre-mix of enzyme plus inhibitor is incubated for 1 h and then added to a GSKα peptide (Ac-KKGGRARTSS-FAEPG-amide) and [γ33P] ATP. Reactions are terminated after 2 h and the radio labeled AKT peptide product is captured in a phospho-cellulose filter plate. Progress curve analysis utilizes continuous real-time fluorescence detection of product formation using the Sox-AKT-tide substrate (Ac-ARKRERAYSF-d-Pro-Sox-Gly-NH2).

Cell Research: A 3-day proliferation assay using CellTiter-Glo is performed to measure the growth inhibition by the compounds at 0-30 μM. Cell growth is determined relative to untreated (DMSO) controls. EC50's are calculated from inhibition curves using a 4- or 6-parameter fitting algorithm in the Assay Client application.(Only for Reference)

Chemical Properties

Molecular Weight: 427.32

Formula: C18H17Cl2FN4OS

CAS No.: 1047644-62-1

Storage & Solubility Information

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 79 mg/mL (184.9 mM)

Ethanol: 79 mg/mL (184.9 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Catalog #: T1911

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References and Literature

1. Dumble M, et al. PLoS One, 2014, 9(6):e100880.

2. Wang J, Xu X, Wang T, et al. Ceritinib increases sensitivity of AKT inhibitors to gastric cancer[J]. European Journal of Pharmacology. 2021: 173879.