AZD-26

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZD-26 是一种变构 AKT 抑制剂 (IC50: 1.04 μM)。

AZD-26 is an inhibitor of AKT.

AKT-IN-1 is able to potently inhibit phosphorylation of AKT in cells at both Thr308 and Ser473, with IC50s of 0.422 and 0.322 μM, respectively. AKT-IN-1 inhibits the phosphorylation of ribosomal protein S6, a downstream effector of the PI3K-AKT pathway. AKT-IN-1 potently inhibits the phosphorylation of PRAS40.

The effects of AKT-IN-1 (Compound 26) in vivo are characterized by measuring the pharmacodynamic activity of AKT-IN-1 in a BT474c breast adenocarcinoma xenograft model. Following acute doses of 100 and 200 mg/kg, AKT-IN-1 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 AKT-IN-1 is further characterized by measuring the effects on the growth of tumor cell xenografts. Continuous (daily) oral dosing of AKT-IN-1 (100 and 200 mg/kg) to nude mice bearing BT474c breast adenocarcinoma xenografts results in inhibition of tumor growth in a dose-dependent manner. When dosed at 200 mg/kg daily, AKT-IN-1 causes significant tumor growth inhibition.

AZD-26 | AZD 26 | AZD26

Others

Other Targets

allosteric Akt

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1357158-81-6

343.42

C22H21N3O

>98% (HPLC)

DMSO : 25 mg/mL 72.80 mM;

NC1(CCC1)c2ccc(cc2)c3ncc(cc3c4ccccc4)C(N)=O

6-[4-(1-Aminocyclobutyl)phenyl]-5-phenylpyridine-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years