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FRAX1036 (Free base)

(CAS No:1432908-05-8)
FRAX-1036 is a potent and selective PAK1 inhibitor.
CAS No:1432908-05-8
Molecular Weight(MW):518.05
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 1432908-05-8
Molecular formula(MF) C28H32ClN7O
Molecular Weight(MW): 518.05
Alias
Solubility
In vitro Ethanol 20 mg/mL (38.6 mM)
DMSO <1 mg/mL
Water <1 mg/mL
In vivo
Biological Activity
Description FRAX-1036 is a potent and selective PAK1 inhibitor.
Targets
PAK1 [1] PAK2 [1] PAK4 [1]
23.3 nM(Ki) 72.4 nM(Ki) 2.4 μM(Ki)
In vitro

Potent cellular inhibition of group I PAK substrate phosphorylation (MEK1-S298 and CRAF-S338) was observed at 2.5 to 5 μM concentrations of FRAX1036 in PAK1-amplified MDA-MB-175 cells. Treatment of PAK1-amplified breast cancer cells with FRAX1036 results in apoptosis[1]. And treatment of OVCAR-3 cells with FRAX-1036 results in upregulation of p53 and p21, while down-regulating cyclin B1[3].

In vivo Treatment with Frax1036 results in slower KT21 tumor growth and is unlikely to have significant blood brain barrier permeability in mice[4].