首页 Cytoskeletal Signaling PAK FRAX597
FRAX597
编号 T6014    
CAS 1286739-19-2     分子式 C29H28ClN7OS     分子量 558.1
靶点: PAK1; PAK2; PAK3;
FRAX597 is an effective, ATP-competitive inhibitor of group I PAKs, and for PAK1(IC50=8 nM), PAK2(IC50=13 nM), and PAK3 (IC50=19 nM).
选择批次  
规格 库存 单价 数量
2 mg 上海现货 485.00
5 mg 上海现货 935.00
10 mg 上海现货 1565.00
50 mg 上海现货 4625.00
100 mg 上海现货 7775.00
1 mL * 10 mM (in DMSO) 上海现货 1140.00
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生物活性

产品描述

FRAX597 is an effective, ATP-competitive inhibitor of group I PAKs, and for PAK1(IC50=8 nM), PAK2(IC50=13 nM), and PAK3 (IC50=19 nM).

靶点活性

PAK1,8nM

PAK2,13nM

PAK3,19nM

体外活性

FRAX597抗野生型PAK1(IC50=48 nM),而抗V342F PAK1突变型(IC50>3 μM)和V342Y PAK1突变型(IC50>2 μM)。FRAX597(100 nM )对YES1 (87%),RET (82%),CSF1R (91%),TEK (87%),PAK1 (82%),和PAK2 (93%)表现出明显的抑制作用。

体内活性

负荷Nf2-/-SC4 Schwann细胞的NOD/SCID小鼠中,每天口服 FRAX597(100 mg/kg),对肿瘤生长有明显的抑制作用.患有原位脑膜瘤的SCID小鼠中,每天口服 FRAX597(90 mg/kg),明显抑制肿瘤生长.在KrasG12D小鼠中,每天口服 FRAX597(90 mg/kg),处理引起肿瘤消退以及Erk与Akt活性损失.

激酶实验

Determination of Enzyme IC50 Values: IC50 values are determined using a 10 concentration point, non-radioactive, functional assay that employs a fluorescence-based, coupled-enzyme format, according to the manufacturer’s protocol (Z’-LYTE@biochemical assay). Kinase selectivity is determined using both the Z’-LYTE@ and Adapta@ kinase assay format.

细胞实验

30,000 cells/well are plated in 12-well dishes in triplicate. Cell growth media with or without FRAX597 is replaced daily. At indicated time points, cells from individual wells are trypsinized and counted using a Coulter counter.(Only for Reference)

细胞系: SC4 cells

动物实验

动物模型:SCID mice with orthotopic meningioma model

化学信息

分子量

558.1

分子式

C29H28ClN7OS

CAS

1286739-19-2

溶解度

DMSO: 11.2 mg/mL (20 mM)

( < 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 1.792 ml 8.959 ml 17.918 ml
5 mM 0.358 ml 1.792 ml 3.584 ml
10 mM 0.179 ml 0.896 ml 1.792 ml
50 mM 0.036 ml 0.179 ml 0.358 ml
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