Afuresertib hydrochloride
Based on 20 publication(s) in Google Scholar
Afuresertib hydrochloride (GSK 2110183 hydrochloride) is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor with Kis of 0.08/2/2.6 nM for Akt1/Akt2/Akt3 respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.95%
- No. CAS: 1047645-82-8
- Fòrmula: C18H18Cl3FN4OS
- Peso molecular:463.78
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Afuresertib hydrochloride
More- Cell. 2024 Feb 1;187(3):624-641.e23. [Abstract]
- Sci Transl Med. 2021 Jan 27;13(578):eaba7308. [Abstract]
- Theranostics. 2019 Jan 30;9(4):1096-1114. [Abstract]
- Genes Dis. 2021 Aug 17;9(2):562-575. [Abstract]
- Cell Syst. 2018 Apr 25;6(4):424-443.e7. [Abstract]
- Molecules. 2019 Apr 1;24(7):1260. [Abstract]
- Sci Rep. 2026 Jan 25;16(1):6197. [Abstract]
- Int J Cancer. 2020 Apr 1;146(7):1963-1978. [Abstract]
- Cancers (Basel). 2022 May 19;14(10):2493. [Abstract]
- J Physiol. 2017 Jul 1;595(13):4207-4225. [Abstract]
- J Biol Chem. 2024 Feb;300(2):105641. [Abstract]
- Food Chem Toxicol. 2025 Oct:204:115628. [Abstract]
- J Cell Biochem. 2024 Aug;125(8):e30613. [Abstract]
- The University of Texas Health Science Center at San Antonio. 2026.
- Biomed Pharmacother. 2025 Nov:192:118707. [Abstract]
- bioRxiv. 2025 Jun 16.
- Patent. US20230147129A1.
- Research Square Print. October 27th, 2022.
- Cold Spring Harb Mol Case Stud. 2022 Jan 10;8(1):a006140. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
Customer Validation & Images
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Flow Cytometry
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Flow Cytometry
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WB
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Cell Proliferation/Viability Assay
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WB
Actividad biológica
Descripciòn
IC50 & Target
[2]|
Akt1 0.08 nM (Ki) |
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) |
ROCK 100 nM (IC50) |
PKCθ 510 nM (IC50) |
In Vitro
Afuresertib (GSK 2110183) 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 p21WAF1/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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1047645-82-8
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Appearance Solid
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Peso molecular 463.78
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Fòrmula C18H18Cl3FN4OS
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Color White to yellow
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SMILES
O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN.[H]Cl
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Synonyms
GSK2110183 hydrochloride; LAE002 hydrochloride
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-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 (20)
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Journal Impact Factor
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Most Recent
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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
Afuresertib hydrochloride purchased from MedChemExpress. Usage Cited in: Cell. 2024 Feb 1;187(3):624-641.e23. [Abstract]
Representative flow cytometry plots of the percentage of ILC2 cell death in the absence or presence of a FOXO1 inhibitor (AS1842856, 50 nM) or an AKT inhibitor (afuresertib, 1 μM).
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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
Afuresertib hydrochloride purchased from MedChemExpress. Usage Cited in: Theranostics. 2019 Jan 30;9(4):1096-1114. [Abstract]
Alterations in RAS signaling induced by the AKT inhibitor GSK2110183 (10 nM; 8 h).
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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
Afuresertib hydrochloride purchased from MedChemExpress. Usage Cited in: Genes Dis. 2021 Aug 17;9(2):562-575. [Abstract]
iTreg cells from cKO/control mice were treated with DMSO, afuresertib (AFU) or MK-2206 (MK). Flow cytometric detection of FoxP3 after gating on CD4+ T cells. Statistical chart showing the proportion of iTreg cells.
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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 -
Molecules
Screening of PI3K-Akt-targeting Drugs for Silkworm against Bombyx mori Nucleopolyhedrovirus. [Abstract]2019 Apr 1;24(7):1260. PMID: 30939726 -
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 -
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 -
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 hydrochloride 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.
Afuresertib hydrochloride purchased from MedChemExpress. Usage Cited in: J Physiol. 2017 Jul 1;595(13):4207-4225. [Abstract]
The levels of pS6K1, p4E-BP1, and pGSK3β in the brain cortical homogenate of untreated or AKT inhibitor, Afuresertib (Afu)-treated WT and Cln1−/− mice (n = 5). AKT inhibitors, Afuresertib (Afu 50 mg/kg body weight and Uprosertib (Upr 50 mg/kg body weight) for 2 weeks.
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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
2024 Aug;125(8):e30613. PMID: 38860522 -
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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 -
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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
2018:1711:351-398. PMID: 29344898
Solvente y solubilidad
In Vitro:
DMSO : 250 mg/mL (539.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 12.5 mg/mL (26.95 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.39 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.39 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
Pureza y Documentación
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Ficha de datos (283 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.1562 mL | 10.7810 mL | 21.5619 mL | 53.9049 mL |
| 5 mM | 0.4312 mL | 2.1562 mL | 4.3124 mL | 10.7810 mL | |
| 10 mM | 0.2156 mL | 1.0781 mL | 2.1562 mL | 5.3905 mL | |
| 15 mM | 0.1437 mL | 0.7187 mL | 1.4375 mL | 3.5937 mL | |
| 20 mM | 0.1078 mL | 0.5390 mL | 1.0781 mL | 2.6952 mL | |
| 25 mM | 0.0862 mL | 0.4312 mL | 0.8625 mL | 2.1562 mL | |
| DMSO | 30 mM | 0.0719 mL | 0.3594 mL | 0.7187 mL | 1.7968 mL |
| 40 mM | 0.0539 mL | 0.2695 mL | 0.5390 mL | 1.3476 mL | |
| 50 mM | 0.0431 mL | 0.2156 mL | 0.4312 mL | 1.0781 mL | |
| 60 mM | 0.0359 mL | 0.1797 mL | 0.3594 mL | 0.8984 mL | |
| 80 mM | 0.0270 mL | 0.1348 mL | 0.2695 mL | 0.6738 mL | |
| 100 mM | 0.0216 mL | 0.1078 mL | 0.2156 mL | 0.5390 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Afuresertib hydrochloride Related Classifications
HY-15727A Related Classifications
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