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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $115 | In Stock | |
2 mg | $161 | In Stock | |
5 mg | $247 | In Stock | |
10 mg | $422 | In Stock | |
25 mg | $687 | In Stock | |
50 mg | $957 | In Stock | |
100 mg | $1,290 | In Stock | |
1 mL x 10 mM (in DMSO) | $198 | 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]. |
Alias | AZD26, AZD-26, AZD 26 |
Molecular Weight | 343.42 |
Formula | C22H21N3O |
Cas No. | 1357158-81-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 11 mg/mL (32.03 mM), Sonication is recommended. ![]() | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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