CAS:1191951-57-1PHT-427

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Synonyms: CS-0223

PHT-427 is dual inhibitor of Akt and PDPK1 with Ki of 2.7 μM and 5.2 μM, respectively, targeting PH domains of Akt and PDPK1.

规格	价格	促销价格	库存

18817579266

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18817579266

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实验数据

技术信息

CAS号

1191951-57-1

储存条件

分子式

C20H31N3O2S2

运输

蓝冰

分子量

409.61

别名

CS-0223

溶解度

动物实验配方

5% DMSO+95% Corn oil

5 mg/mL

生物活性

靶点 Akt

Ki:2.7μM PDK-1

Ki:5.2μM
描述Phosphatidylinositol 3-kinase (PIK3)/PtdIns dependent protein kinase-1(PDPK1)/Akt signaling plays a critical role in activating proliferation and survival pathways within cancer cells. PHT-427 is a compound designed to bind to the pleckstrin homology (PH) binding domain of signaling molecules. PHT-427 itself (C-12 chain) bound with the highest affinity to the PH domains of both PDPK1 and Akt. PHT-427 inhibited Akt and PDKP1 signaling and their downstream targets in sensitive but not resistant cells and tumor xenografts. The Ki values of PHT-427 are 2.7 and 5.2 µM towards Akt and PDPK1 respectively. RPPA studies in PC-3 prostate cancer cells showed that PHT-427 caused a reduction in phospho-Thr³⁰⁸-Akt, and also in phospho-Ser²⁴¹-PDPK1 and its downstream targets, phospho-Ser⁶⁵⁷-PKC and total SGK1. In vivo studies in mice with BxPC-3 and MiaPaCa-2 xenografts treated with a 200 mg/kg dose of PHT-427 showed a decrease in phospho-Ser⁴⁷³-AKT, phospho-Thr³⁰⁸-Akt, phospho-Ser²⁴¹-PDPK1 and in the PDKP1-specific downstream target phospho-Ser²²¹-RSK.
动物研究
剂量
Mice: 200 mg/kg^[3] (p.o.); 10 mg/kg^[4] (i.p.)

给药途径
p.o., i.p.

靶点	Description	IC50
Akt		Ki:2.7μM
PDK-1		Ki:5.2μM