| 供货周期： | 一周 |
| 品牌： | 爱必信 |
| 规格： | >98% |
| 货号： | abs813269 |
| CAS号： | 1191951-57-1 |
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抑制剂描述： 产品名称：PHT-427 产品别名：见爱必信官网 英文别名：PHT-427 靶点：Akt CAS：1191951-57-1 纯度：>98% 外观：见爱必信官网 保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述： PHT-427是作用于Akt和PDPK1的双重抑制剂，Akt和PDPK1的PH结构域具有高度亲和力，Ki分别为2.7 μM和5.2 μM。PH-427是Akt/PDPK1的血小板白细胞C 激酶底物同源性（PH）域抑制剂。10 μM PH-427作用于PC-3前列腺癌细胞，显著降低p-Ser241-PDPK1和p-Thr308-Akt,说明PHT-427可抑制 Akt 和PDKP1。 PHT-427 作用于质膜，也抑制Akt 和 PDKP1 PH 域易位。 溶解性：DMSO ：41 mg/mL (100 mM) 体外研究： PH-427 is a pleckstrin homology domain inhibitor to Akt/PDPK1. PH-427 significantly reduces phospho-Ser241-PDPK1 phospho-Thr308-Akt in PC-3 prostate cancer cells at 10 μM, which shows that PHT-427 could inhibit both Akt and PDPK1. PHT-427 also inhibits translocation of the Akt and PDPK1 PH domains in plasma membrane. PHT-427 induces apoptosis and inhibits AKT phosphorylation with IC50 of 8.6 μM (in BxPC-3 cells), which mainly on its Ser473 residue and less strongly on Thr308 residue without affecting total Akt protein expression. PHT-427 also shows antiproliferation in Panc-1 cells with IC50 of 65 μM. 体内研究：PHT-427 shows great antitumor activity in BxPC-3 pancreatic, MCF-7 breast and A-549 NSCL cancer xenografts. PHT-427 gives up to an 80% inhibition of tumor growth in BxPC-3 at doses of 125 to 250 mg/kg.
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