Art. -Nr.: HY-15727

Afuresertib

(Synonyms: GSK2110183; LAE002)

19 Cited Publications

Kundenbewertung

Based on 19 publication(s) in Google Scholar

Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K_is of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively.

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Reinheit: 99.53%
CAS. Nr.: 1047644-62-1
Formel: C₁₈H₁₇Cl₂FN₄OS
Molecular Weight:427.32

Speicherung:

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Afuresertib Chemical Structure

CAS. Nr.: 1047644-62-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (19)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Afuresertib (GSK2110183) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with K_is of 0.08/2/2.6 nM for Akt1/Akt2/Akt3, respectively^[1]^[2].

IC₅₀ & Target^[1]

Akt2

2 nM (Ki)

Akt3

2.6 nM (Ki)

Akt1 E17K mutant

0.2 nM (IC₅₀)

PKCη

210 nM (IC₅₀)

PKC-βI

430 nM (IC₅₀)

PKCθ

510 nM (IC₅₀)

ROCK

100 nM (IC₅₀)

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle PKC Isoform-spezifische Produkte anzeigen :

Alle ROCK Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H358	IC₅₀	<0.1 μM Compound: A1-NH2	Antiproliferation activity against human NCI-H358 cells incubated for 3 days in presence of trametinib by MTT assay Antiproliferation activity against human NCI-H358 cells incubated for 3 days in presence of trametinib by MTT assay	[PMID: 38457912]

In Vitro

Afuresertib (GSK2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G₁ phase. Western blotting analysis shows that Afuresertib increases the expression of p21^WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G₁ phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1047644-62-1
Appearance Solid
Molecular Weight 427.32
Formel C₁₈H₁₇Cl₂FN₄OS
Color White to off-white
SMILES

O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN
Synonyms

GSK2110183; LAE002
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Publications (19)

All Cell Proliferation/Viability Assay

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Journal Impact Factor

Cell

Therapeutic application of human type 2 innate lymphoid cells via induction of granzyme B-mediated tumor cell death. [Abstract]

2024 Feb 1;187(3):624-641.e23. PMID: 38211590
Sci Transl Med

A chimeric antigen receptor with antigen-independent OX40 signaling mediates potent antitumor activity. [Abstract]

2021 Jan 27;13(578):eaba7308. PMID: 33504651
Theranostics

Interaction between p53 and Ras signaling controls cisplatin resistance via HDAC4- and HIF-1α-mediated regulation of apoptosis and autophagy. [Abstract]

2019 Jan 30;9(4):1096-1114. PMID: 30867818
Genes Dis

Protein phosphatase 6 (Pp6) is crucial for regulatory T cell function and stability in autoimmunity. [Abstract]

2021 Aug 17;9(2):562-575. PMID: 35224167
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Biomed Pharmacother

Inhibition of AKT or mTOR molecules mitigates obesity-associated metabolic disorders in Riz1-/- mice with obesity. [Abstract]

2025 Nov:192:118707. PMID: 41151301
Int J Cancer

The NEDD4-1 E3 ubiquitin ligase: A potential molecular target for bortezomib sensitivity in multiple myeloma. [Abstract]

2020 Apr 1;146(7):1963-1978. PMID: 31390487
Molecules

Screening of PI3K-Akt-targeting Drugs for Silkworm against Bombyx mori Nucleopolyhedrovirus. [Abstract]

2019 Apr 1;24(7):1260. PMID: 30939726
Cancers (Basel)

RON ( MST1R) and HGFL ( MST1) Co-Overexpression Supports Breast Tumorigenesis through Autocrine and Paracrine Cellular Crosstalk. [Abstract]

2022 May 19;14(10):2493. PMID: 35626096
J Physiol

Angiotensin II activates CaV 1.2 Ca2+ channels through β-arrestin2 and casein kinase 2 in mouse immature cardiomyocytes. [Abstract]

2017 Jul 1;595(13):4207-4225. PMID: 28295363

Afuresertib purchased from MedChemExpress. Usage Cited in: J Physiol. 2017 Jul 1;595(13):4207-4225. [Abstract]

Effects of pharmacological inhibitors on AngII-mediated activation of L-type Ca²⁺ channels in NVCMs. NVCMs are treated with vehicle, Erlotinib, H-89, Afuresertib (1 μM), Gö6983, CID755673, KN-93, SCH772984, Bosutinib or Quinalizarin for 30 min before treatment of AngII.
Sci Rep

Targeting the Akt-EphA2 axis and cell-cell adhesion enhances anoikis sensitivity in cancer cells. [Abstract]

2026 Jan 25;16(1):6197. PMID: 41582276
J Biol Chem

Disruption of lysosomal nutrient sensing scaffold contributes to pathogenesis of a fatal neurodegenerative lysosomal storage disease. [Abstract]

2024 Feb;300(2):105641. PMID: 38211816
Food Chem Toxicol

Mechanistic insights into AKT1/GSK3β/CD36 axis regulation in ZLY06-induced hepatic lipid metabolism dysfunction and protective intervention via AKT activation strategies. [Abstract]

2025 Oct:204:115628. PMID: 40633829
J Cell Biochem

AKT1 Promotes Tumorigenesis and Metastasis by Directly Phosphorylating Hexokinases. [Abstract]

2024 Aug;125(8):e30613. PMID: 38860522
bioRxiv

2025 Jun 16.
Patent

US20230147129A1.
Research Square Print

October 27th, 2022.
Cold Spring Harb Mol Case Stud

Functional impact and targetability of PI3KCA, GNAS, and PTEN mutations in a spindle cell rhabdomyosarcoma with MYOD1 L122R mutation. [Abstract]

2022 Jan 10;8(1):a006140. PMID: 35012940
Methods Mol Biol

Methods for High-throughput Drug Combination Screening and Synergy Scoring. [Abstract]

2018:1711:351-398. PMID: 29344898

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (234.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3402 mL

11.7008 mL

23.4017 mL

5 mM

0.4680 mL

2.3402 mL

4.6803 mL

10 mM

0.2340 mL

1.1701 mL

2.3402 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (5.85 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.85 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Cell Assay^[1]

MPM cells are seeded in 96-well plates (cell density, 2.5×10³ cells/well) and are incubated for 24 h at 37°C. Next, the cells are incubated in a medium containing indicated concentrations of Akt inhibitors (e.g., Afuresertib ; 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM) for 72 h. Next, MTT solution is added to each well, and the cells are incubated for 4 h. Finally, the cells are incubated overnight with lysis buffer (10% SDS in 0.01 mol/L hydrogen chloride). Absorbance is measured at 550 nm using SpectraMAX M5 spectrophotometer^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Yamaji M, et al. Novel ATP-competitive Akt inhibitor Afuresertib suppresses the proliferation of malignant pleural mesothelioma cells. Cancer Med. 2017 Nov;6(11):2646-2659. [Content Brief]

[2]. Dumble M, et al. Discovery of novel AKT inhibitors with enhanced anti-tumor effects in combination with the MEK inhibitor. PLoS One. 2014 Jun 30;9(6):e100880 [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3402 mL	11.7008 mL	23.4017 mL	58.5042 mL
	5 mM	0.4680 mL	2.3402 mL	4.6803 mL	11.7008 mL
	10 mM	0.2340 mL	1.1701 mL	2.3402 mL	5.8504 mL
	15 mM	0.1560 mL	0.7801 mL	1.5601 mL	3.9003 mL
	20 mM	0.1170 mL	0.5850 mL	1.1701 mL	2.9252 mL
	25 mM	0.0936 mL	0.4680 mL	0.9361 mL	2.3402 mL
	30 mM	0.0780 mL	0.3900 mL	0.7801 mL	1.9501 mL
	40 mM	0.0585 mL	0.2925 mL	0.5850 mL	1.4626 mL
	50 mM	0.0468 mL	0.2340 mL	0.4680 mL	1.1701 mL
	60 mM	0.0390 mL	0.1950 mL	0.3900 mL	0.9751 mL
	80 mM	0.0293 mL	0.1463 mL	0.2925 mL	0.7313 mL
	100 mM	0.0234 mL	0.1170 mL	0.2340 mL	0.5850 mL

Keywords

Afuresertib

19 Cited Publications

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Afuresertib

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

TGF-beta/Smad Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Coagulation and Anti-coagulation Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Extracellular Vesicles (EVs) Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Epigenetics Compound Library Mini

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Afuresertib

Alle Akt Isoform-spezifische Produkte anzeigen

Alle PKC Isoform-spezifische Produkte anzeigen

Alle ROCK Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (19)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Afuresertib Related Classifications

HY-15727 Related Classifications