供货周期: | 一周 |
品牌: | 爱必信 |
规格: | >98% |
货号: | abs811837 |
CAS号: | 1643913-93-2 |
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抑制剂描述: 产品名称:KPT-9274 产品别名:见爱必信官网 英文别名:KPT-9274 靶点:PAK CAS:1643913-93-2 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: KPT-9274 is an orally bioavailable small molecule that is a non-competitive dual inhibitor of PAK4 and NAMPT. It shows an IC50 of ~120 nM for NAMPT in a cell-free enzymatic assay. 溶解性:DMSO: ≥ 32 mg/mL 体外研究: KPT-9274 interferences with PAK4 and NAD biosynthetic pathways results in reduction of G2/M transit as well as induction of apoptosis and decrease in cell invasion and migration in several human RCC cell lines. The inhibition of the PAK4 pathway by KPT-9274 attenuates nuclear β-catenin as well as the Wnt/β-catenin targets cyclin D1 and c-Myc. 体内研究:KPT-9274 administration to a 786-O (VHL-mut) human RCC xenograft model leads to dose-dependent inhibition of tumor growth with no apparent toxicity. It also shows remarkable anti-tumor activity in sub-cutaneous xenograft models of pancreatic ductal adenocarcinoma (PDAC) cell lines and cancer stem cells as a single agent. KPT-9274 possesses desirable PK properties and is well tolerated in mice with the absence of any signs of toxicity when 200 mg/kg daily is administered either intravenously or orally.
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