FRAX1036 是一种有效的选择性 PAK1 抑制剂，对 PAK1、PAK2 和 PAK4 的Ki值分别为 23.3 nM、72.4 nM 和 2.4 μM。

FRAX-1036 is a effective and selective PAK1 inhibitor.

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.

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

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

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

1432908-05-8

C28H32ClN7O

518.06

DMSO:insoluble
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