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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
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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Purity 97.51%

HNMR HPLC COA Datasheet MSDS

Purity 98.00%

HNMR COA Datasheet MSDS

Purity 99.77%

HNMR HPLC COA Datasheet MSDS

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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Answers to questions you may have can be found in the Inhibitor Handling Instructions. Topics include how to prepare stock solutions, how to store Products, and issues that need special attention for cell-based assays and animal experiments.

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.