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Afuresertib

Catalog No. T1911 CAS 1047644-62-1

Synonyms: GSK2110183C, GSK2110183

Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.

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Afuresertib, CAS 1047644-62-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 33.00
2 mg	In stock	$ 46.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 178.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 503.00
500 mg	In stock	$ 1,090.00
1 mL * 10 mM (in DMSO)	In stock	$ 72.00

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Purity: 99.77%

Purity: 98.85%

Purity: 98%

Purity: 97.51%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Afuresertib (GSK2110183) is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity.
Targets&IC50	Akt1:0.08 nM(Ki), Akt2:2 nM(Ki), Akt3:2.6 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)

Synonyms	GSK2110183C, GSK2110183
Molecular Weight	427.32
Formula	C18H17Cl2FN4OS
CAS No.	1047644-62-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 79 mg/mL (184.9 mM)

Ethanol: 79 mg/mL (184.9 mM)

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.

Citations

1. Wang J, Xu X, Wang T, et al. Ceritinib increases sensitivity of AKT inhibitors to gastric cancer. European Journal of Pharmacology. 2021: 173879. 2. Wang J, Xu X, Wang T, et al. Ceritinib increases sensitivity of AKT inhibitors to gastric cancer. European Journal of Pharmacology. 2021: 173879. 3. Huang Q, Ru Y, Luo Y, et al.Identification of a targeted ACSL4 inhibitor to treat ferroptosis-related diseases.Science Advances.2024, 10(13): eadk1200.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Active Compound Library Drug Repurposing Compound Library TGF-beta/Smad Compound Library Anti-Cancer Clinical Compound Library Kinase Inhibitor Library Anti-Cancer Drug Library NO PAINS Compound Library Metabolism Compound Library Anti-Breast Cancer Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Afuresertib 1047644-62-1 Cell Cycle/Checkpoint Chromatin/Epigenetic Cytoskeletal Signaling PI3K/Akt/mTOR signaling Stem Cells ROCK PKC Akt ROK Rho-associated kinase Rho-kinase Inhibitor Rho-associated protein kinase GSK-2110183 GSK2110183C inhibit PKB GSK 2110183 GSK2110183 Protein kinase C Protein kinase B inhibitor

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