| Field | Specification |
|---|---|
| Target | |
| Alternative names | GSK2110183 hydrochloride; LAE002 hydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H18Cl3FN4OS |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Afuresertib hydrochloride is an orally bioavailable, selective, ATP-competitive and potent pan-Akt kinase inhibitor, with Ki values of 0.08, 2 and 2.6 nM against Akt1, Akt2 and Akt3, respectively[1][2]. Also known as GSK2110183 hydrochloride and LAE002 hydrochloride, it is supplied as a white to yellow solid (C18H18Cl3FN4OS, MW 463.78) at 99.95% purity.
Physical & Chemical Properties
| CAS Number | 1047645-82-8 |
|---|---|
| Molecular Formula | C18H18Cl3FN4OS |
| Molecular Weight | 463.78 g/mol |
| Purity | 99.95% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(F)=C3)CN.[H]Cl |
| Target | Akt1, Akt2, Akt3, Akt1 E17K mutant, PKCη, PKC-βI, ROCK, PKCθ |
| Signaling Pathway | PI3K/Akt/mTOR; TGF-beta/Smad; Epigenetics; Cell Cycle/DNA Damage; Stem Cell/Wnt; Cytoskeleton |
| Solubility | In Vitro: DMSO: 250 mg/mL (539.05 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 12.5 mg/mL (26.95 mM; Requires sonication) |
| Storage | -20°C, protect from light, stored under nitrogen. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
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) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 250 mg/mL (539.05 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 12.5 mg/mL (26.95 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light, stored under nitrogen; avoid repeated freeze-thaw cycles.
If water is used as the stock solvent, dilute to the working solution and sterilize it through a 0.22 μm filter before use.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.5 mg/mL (5.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 2.5 mg/mL (5.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.5 mg/mL (5.39 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (25.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
Afuresertib (GSK 2110183) shows favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. In ACC-MESO-4 and MSTO-211H cells, Afuresertib significantly raises caspase-3 and caspase-7 activities and the number of apoptotic cells. Afuresertib strongly arrests the cell cycle in G1 phase. Western blotting shows that Afuresertib raises p21WAF1/CIP1 expression and lowers phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-driven p21 expression promotes arrest in G1 phase through induction of FOXO activity. Cisplatin-induced cytotoxicity is significantly enhanced by Afuresertib. Afuresertib alters expression of E2F1 and MYC, which are associated with the fibroblast core serum response[1].
In Vivo
Mice with BT474 breast tumor xenografts receive daily oral doses of vehicle or GSK2110183 (10, 30 or 100 mg/kg) for 21 days, giving 8, 37 and 61% TGI, respectively. GSK2110183 is well tolerated by the mice, with 1-3% body weight loss reported after 5 days of dosing that recovers during the study. Further tumor xenograft models with Akt pathway activation are examined to demonstrate compound efficacy. In SKOV3 xenografts, treatment with GSK2110183 at 10, 30 and 100 mg/kg gives 23, 37 and 97% TGI, respectively[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Seed MPM cells in 96-well plates (cell density, 2.5×103 cells/well) and incubate for 24 h at 37°C. Then incubate the cells for 72 h in medium with the indicated concentrations of Akt inhibitors (for example Afuresertib; 50, 20, 10, 5, 2, 1, 0.5, 0.2, 0.1, and 0.01 μM). Add MTT solution to each well and incubate the cells for 4 h. Finally, incubate the cells overnight with lysis buffer (10% SDS in 0.01 mol/L hydrogen chloride). Measure absorbance at 550 nm with a SpectraMAX M5 spectrophotometer[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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