FRAX597

Description	in vitro: FRAX597 was determined to be a potent, ATP competitive inhibitor of group I PAKs (PAK 1-3)，with biochemical IC50 values as follows: PAK1 IC50 = 8 nM , PAK2 IC50 = 13 nM, PAK3 IC50= 19 nM.The IC50 towards PAK4, a member of group II PAKs was >10mM. To determine the cellular IC50 values for FRAX597, SC4 Schwann cells (Nf2-null Schwann cells) were treated with an escalating dose of FRAX597. PAK1 activation requires an autophosphorylation step and thus the activity of PAK1 was determined by western blot analysis using an antibody against phospo(Ser144)-PAK1. These studies establish an approximate IC50 of 70 nM for FRAX597 in culture . in vivo: Ten days post injection, similar flux readings for all animals were validated and animals were enrolled randomly into control (vehicle only) or drugtreated cohorts (100mg/kg, oral, once daily) for a period of 14 days. Analysis of the flux reading for the animals in the two cohorts demonstrated a significantly slower tumor growth rate in FRAX
Pathways	Cell Cycle/DNA Damage
Targets	PAK

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