FRAX597 是一种有效的 ATP 竞争性 I 组 PAK 抑制剂，作用于PAK1、2和3，IC50分别为 8、13 和 19 nM。

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).

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.

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。

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.

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)

1286739-19-2

C29H28ClN7OS

558.1

DMSO:11.2 mg/mL (20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years