化合物KPT9274 T4354

Product Introduction
Bioactivity


英文名: KPT9274

描述: KPT9274 (PAK4-IN-1) 是一种非竞争性的 PAK4 和 NAMPT 双重抑制剂（IC50= ~120 nM）。它是一种口服生物可利用的小分子。

细胞实验: 786-0, ACHN, Caki-1 and U-2 OS cells are treated with KPT-9274 (1 μM and 5 μM) incubating for 12 hours.

动物实验: 786-O (VHL-mut) human RCC xenograft model (nude mice) is treated with KPT-9274 (100 and 200 mg/kg),prepared in 58% Polyvinylpyrrolidone K30 + 21% methyl cellulose + 21% Phospholipon 90 g, by oral gavage.

体外活性: In several human RCC cell lines, KPT-9274 interferences with PAK4 and NAD biosynthetic pathways leading to reduction of G2/M transit as well as induction of apoptosis and decrease in cell invasion and migration. 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.

体内活性: In mice, KPT-9274 (200 mg/kg) daily is administered either intravenously or orally with the absence of any signs of toxicity.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 55 mg/mL (90.07 mM)


关键字: KPT9274

相关产品: NAMPT degrader-3 | Nampt activator-1 | SBI-797812 | Nampt-IN-1 | LB-60-OF61 | CHS-828 | (E)-Daporinad | Nampt-IN-5 | OT-82 | Teglarinad chloride

相关库: Drug Repurposing Compound Library | Glycometabolism Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途