首页 Metabolism NAMPT KPT9274
KPT9274
编号 T4354     别名: KPT 9274, KPT-9274, PAK4-IN-1, PAK4-IN-1, KPT-9274 KPT 9274
CAS 1643913-93-2     分子式 C35H29F3N4O3     分子量 610.64
靶点: NAMPT; PAK4;
KPT-9274 is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.
选择批次  
规格 库存 单价 数量
2 mg 上海现货 1231.00
5 mg 上海现货 2217.00
10 mg 上海现货 3990.00
25 mg 上海现货 6600.00
50 mg 上海现货 11667.00
100 mg 上海现货 18867.00
1 mL * 10 mM (in DMSO) 上海现货 3990.00
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生物活性

产品描述

KPT-9274 is a non-competitive dual inhibitor of PAK4 and NAMPT(IC50= ~120 nM). It is an orally bioavailable small molecule.

靶点活性

NAMPT,

PAK4,

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.

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 90G, by oral gavage.

细胞实验

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

化学信息

分子量

610.64

分子式

C35H29F3N4O3

CAS

1643913-93-2

溶解度

DMSO: 32 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.638 ml 8.188 ml 16.376 ml
5 mM 0.328 ml 1.638 ml 3.275 ml
10 mM 0.164 ml 0.819 ml 1.638 ml
50 mM 0.033 ml 0.164 ml 0.328 ml
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