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AKT-IN-1 Sale

(Synonyms: 6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺) 目录号 : GC33308

AKT-IN-1是一种变构AKT抑制剂,IC50为1.042μM。

AKT-IN-1 Chemical Structure

Cas No.:1357158-81-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,700.00
现货
5mg
¥2,250.00
现货
10mg
¥4,050.00
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25mg 待询 待询
50mg 待询 待询
100mg 待询 待询

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Sample solution is provided at 25 µL, 10mM.

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产品描述

AKT-IN-1 is an allosteric AKT inhibitor with an IC50 of 1.042 μM.

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[1].

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[1].

[1]. Kettle JG, et al. Diverse heterocyclic scaffolds as allosteric inhibitors of AKT. J Med Chem. 2012 Feb 9;55(3):1261-73.

Chemical Properties

Cas No. 1357158-81-6 SDF
别名 6-[4-(1-氨基环丁基)苯基]-5-苯基-3-吡啶甲酰胺
Canonical SMILES NC(C1=CN=C(C2=CC=C(C3(N)CCC3)C=C2)C(C4=CC=CC=C4)=C1)=O
分子式 C22H21N3O 分子量 343.42
溶解度 DMSO : 25 mg/mL (72.80 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 2.9119 mL 14.5594 mL 29.1189 mL
5 mM 0.5824 mL 2.9119 mL 5.8238 mL
10 mM 0.2912 mL 1.4559 mL 2.9119 mL
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