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AKT-IN-1 (AZD-26) is an allosteric AKT inhibitor (IC50: 1.04 μM).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $105 | In Stock | In Stock | |
| 5 mg | $247 | In Stock | In Stock | |
| 10 mg | $422 | In Stock | In Stock | |
| 25 mg | $687 | In Stock | In Stock | |
| 50 mg | $957 | In Stock | In Stock | |
| 100 mg | $1,290 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $198 | In Stock | In Stock |
| Description | AKT-IN-1 (AZD-26) is an allosteric AKT inhibitor (IC50: 1.04 μM). |
| Targets&IC50 | Akt (allosteric):1.04 μM |
| In vitro | AZD-26 is able to potently inhibit phosphorylation of AKT in cells at both Thr308 (IC50: 0.422 μM) and Ser473 (IC50: 0.322 μM). AZD-26 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AZD-26 potently inhibits the phosphorylation of PRAS40 [1]. |
| In vivo | The effects of AZD-26 in vivo are characterized by measuring the pharmacodynamic activity of AZD-26 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AZD-26 potently inhibits the phosphorylation of its downstream substrate GSK3β as well as the phosphorylation of AKT (Ser473), with a potency consistent with its pharmacokinetic profile. The in vivo activity of AZD-26 is further characterized by measuring the effects on the growth of tumour cell xenografts. Continuous (daily) oral dosing of AZD-26 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumour growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AZD-26 causes significant tumour growth inhibition[1]. |
| Synonyms | AZD-26, AZD26, AZD 26 |
| Molecular Weight | 343.42 |
| Formula | C22H21N3O |
| Cas No. | 1357158-81-6 |
| Smiles | NC(=O)c1cnc(-c2ccc(cc2)C2(N)CCC2)c(c1)-c1ccccc1 |
| Relative Density. | 1.210 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 11 mg/mL (32.03 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.82 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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