首页 Cytoskeletal Signaling PAK FRAX1036
FRAX1036
编号 T6839    
CAS 1432908-05-8     分子式 C28H32ClN7O     分子量 518.05
靶点: PAK1; PAK2; PAK4;
FRAX-1036 is a effective and selective PAK1 inhibitor.
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规格 库存 单价 数量
1 mg 上海现货 632.00
5 mg 上海现货 1297.00
10 mg 上海现货 2057.00
50 mg 上海现货 8327.00
100 mg 上海现货 12567.00
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生物活性

产品描述

FRAX-1036 is a effective and selective PAK1 inhibitor.

靶点活性

PAK1,23.3nM(Ki)

PAK2,72.4nM(Ki)

PAK4,2.4μM(Ki)

体外活性

MDA-MB-175 cells,which are PAK1-amplified (MEK1-S298 and CRAF-S338) ,was observed Potent cellular inhibition at 2.5 to 5 μM concentrations of FRAX1036. PAK1-amplified breast cancer cells are treated with FRAX1036 leading to apoptosis. OVCAR-3 cells are treated with FRAX-1036 resulting in upregulation of p53 and p21, while down-regulating cyclin B1.

体内活性

KT21 are treated with Frax1036 showing slower tumor growth, while Frax1036 is unlikely to have significant blood-brain barrier permeability in mice.

细胞实验

MDA-MB175 cells are treated with increasing concentrations (0, 0.5, 1, 2.5, 5 μM) of FRAX1036 for 24 hours.

细胞系: MDA-MB175 cells

动物实验

Pak2-deficient mice were treated by oral gavage of 30 mg/kg Frax1036.

动物模型:Pak2-deficient mice

化学信息

分子量

518.05

分子式

C28H32ClN7O

CAS

1432908-05-8

溶解度

DMSO: 5.3 mg/mL (10.23 mM), Need warming

( < 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 1.93 ml 9.652 ml 19.303 ml
5 mM 0.386 ml 1.93 ml 3.861 ml
10 mM 0.193 ml 0.965 ml 1.93 ml
50 mM 0.039 ml 0.193 ml 0.386 ml
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