| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C20H22Cl3N3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
AT7867 dihydrochloride is a potent, ATP-competitive inhibitor of Akt1, Akt2, and Akt3, with IC50 values of 32 nM, 17 nM, and 47 nM, respectively, and of p70S6K and PKA, with IC50 values of 85 nM and 20 nM, respectively. It is supplied as a white to off-white solid (C20H22Cl3N3, MW 410.77) at 99.73% purity.
Physical & Chemical Properties
| CAS Number | 1431697-86-7 |
|---|---|
| Molecular Formula | C20H22Cl3N3 |
| Molecular Weight | 410.77 g/mol |
| Purity | 99.73% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | ClC1=CC=C(C=C1)C2(CCNCC2)C3=CC=C(C=C3)C4=CNN=C4.[H]Cl.[H]Cl |
| Target | Akt2, p70S6K, Akt1, Akt3, PKA |
| Signaling Pathway | PI3K/Akt/mTOR; TGF-beta/Smad; Stem Cell/Wnt; MAPK/ERK Pathway |
| Solubility | In Vitro: DMSO: 100 mg/mL (243.45 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) H2O: 2.27 mg/mL (5.53 mM; Requires sonication and warming and heat to 60°C) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
Akt2 17 nM (IC50) |
p70S6K 85 nM (IC50) |
Akt1 32 nM (IC50) |
Akt3 47 nM (IC50) |
PKA 20 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 | 100 mg/mL (243.45 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| H2O | 2.27 mg/mL (5.53 mM) | requires sonication and warming and heat to 60°C |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; 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 | ≥ 3.25 mg/mL (7.91 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.25 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (32.5 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 | ≥ 3.25 mg/mL (7.91 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.25 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (32.5 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 | ≥ 3.25 mg/mL (7.91 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 3.25 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 (32.5 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
AT7867 inhibits AKT2 in an ATP-competitive manner, with a Ki of 18nM. It also has potent activity against the structurally related AGC kinases p70S6K and PKA, yet is clearly selective over kinases from other sub-families. In vitro studies of growth inhibition indicate that AT7867 blocks proliferation across a number of human cancer cell lines. Inhibition of proliferation appears most potent in the MES-SA uterine line, the MDA-MB-468 and MCF-7 breast lines, and the HCT116 and HT29 colon lines (IC50 values of 0.9-3 μM), and weakest in the two prostate lines that were tested (IC50 range of 10-12 μM)[1].
In Vivo
After oral administration at 20 mg/kg, AT7867 is eliminated from plasma in a manner that appears similar to that seen after i.v. administration. Plasma levels of AT7867 stay above 0.5 μM for at least 6 hours after an oral dose of 20 mg/kg. Oral bioavailability is calculated at 44%, assuming linear pharmacokinetics after i.v. administration. For this reason, in vivo pharmacodynamic (PD) biomarker studies are carried out with this model. After pharmacokinetic and tolerability studies, AT7867 doses (90 mg/kg p.o. or 20 mg/kg i.p.) are given to athymic mice bearing MES-SA tumors, and the phosphorylation status of GSK3β and S6RP in the tumors is monitored over time. Phosphorylation of both pathway-activity markers is clearly inhibited at 2 and 6 hours after AT7867 treatment. Total levels of both GSK3β and S6RP are greatly reduced by 24 hours[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Cell Assay[1]
Plate cells at 16,000 cells per well in 96-well microplates, using medium containing 10% FBS, and culture for 24 hours before AT7867 treatment. Add AT7867 or vehicle control to the cells for 1 hour. Then fix the cells with 3% paraformaldehyde, 0.25% glutaraldehyde, 0.25% Triton-X100, wash, and block with 5% milk in tris-buffered saline with 0.1% Tween-20 (TBST) before overnight incubation with a phospho-GSK3β (serine 9) antibody. Wash the plates, add secondary antibody, and enhance the signal with DELFIA reagents. Normalize europium counts to the protein concentration, and calculate the IC50 value for each inhibitor using non-linear regression and a sigmoidal dose-response (variable slope) equation in GraphPad Prism[1].
Animal Administration[1]
Mice[1] Use male athymic BALB/c mice (nu/nu). Dose BALB/c mice once with AT7867 at 5 mg/kg intravenously (i.v.) and at 20 mg/kg per os (p.o.). Collect plasma samples from duplicate animals at each of the following time points (0.083, 0.167, 0.33, 0.67, 1, 2, 4, 6, 16 and 24 hours) after i.v. dosing, and 0.25, 0.5, 1, 2, 4, 6 and 24 hours after p.o. dosing. Bleed the mice by cardiac puncture and centrifuge all blood samples to obtain plasma, then freeze at -20°C until analysis. For bioanalysis, prepare all plasma samples by protein precipitation with acetonitrile containing internal standard. Quantify sample extracts by comparison with a standard calibration line constructed with AT7867, using an inhibitor specific liquid chromatography tandem mass spectrometry (LC-MS/MS) method. Determine pharmacokinetic parameters.
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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