Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AKT-IN-1 (AZD-26) is an allosteric AKT inhibitor (IC50: 1.04 μM).
説明 | AKT-IN-1 (AZD-26) is an allosteric AKT inhibitor (IC50: 1.04 μM). |
ターゲット&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]. |
別名 | AZD26, AZD-26, AZD 26 |
分子量 | 343.42 |
分子式 | C22H21N3O |
CAS No. | 1357158-81-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 24 mg/mL, Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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AKT-IN-1 1357158-81-6 Cytoskeletal Signaling PI3K/Akt/mTOR signaling Akt PKB AZD26 AZD-26 inhibit Protein kinase B AKT IN 1 AKTIN1 Inhibitor AZD 26 inhibitor