AKT-IN-1

AKT-IN-1 (AZD-26) 是一种变构的 AKT 抑制剂，其 IC50=1.042 μM。

产品编号 T4489Cas号 1357158-81-6

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纯度:98.02%

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产品编号 T4489别名 AZD26, AZD-26, 6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺, AZD 26Cas号 1357158-81-6

AKT-IN-1 (AZD-26) 是一种变构的 AKT 抑制剂，其 IC50=1.042 μM。

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生物活性

产品描述	AKT-IN-1 (AZD-26) is an allosteric AKT inhibitor (IC50: 1.04 μM).
靶点活性	Akt (allosteric):1.04 μM
体外活性	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].
体内活性	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].
别名	AZD26, AZD-26, 6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺, AZD 26

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

溶解度信息

DMSO: 11 mg/mL (32.03 mM), Sonication is recommended.

溶液配制表

DMSO