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Cytoskeletal Signaling Akt Afuresertib

Afuresertib

Catalog No. T1911   CAS 1047644-62-1
Synonyms: GSK2110183C, GSK2110183

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

Afuresertib, CAS 1047644-62-1
Pack Size Availability Price/USD Quantity
2 mg In stock 50.00
5 mg In stock 80.00
10 mg In stock 110.00
25 mg In stock 198.00
50 mg In stock 320.00
100 mg In stock 560.00
1 mL * 10 mM (in DMSO) In stock 80.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Afuresertib is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
Targets&IC50 Akt1 :ic50 0.08nM(Ki),   Akt2 :ic50 2nM(Ki),   Akt3 :ic50 2.6nM(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)
Cell lines: Hematological cell lines and solid tumor cell lines
Animal Research
Animal Model: Feathymic nude and SCID mice bearing SKOV3 or BT474 tumors
Synonyms GSK2110183C , GSK2110183
Purity 97.51%
Molecular Weight 427.32
Formula C18H17Cl2FN4OS
CAS No. 1047644-62-1

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

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 )

Citations

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

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library PI3K-AKT-mTOR Compound Library Kinase Inhibitor Library Anti-cancer Clinical Compound Library Fluorochemical Library

Related Products

Related compounds with same targets
Karanjin A-674563 2HCl(552325-73-2(fb-2hcl)) Triciribine AT7867 Ilexgenin A Cytochalasin D Pachymic acid Ipatasertib

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