[CAS NO. 1432908-05-8] FRAX1036
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PRODUCTS SPECIFICATIONS [1432908-05-8]
Store
Catalog
SLK-S7989
Brand
Selleck
CAS
1432908-05-8
DESCRIPTION [1432908-05-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 518.05 |
| Molecular Formula | C28H32ClN7O |
| SMILES | O=C1C(C2=CC=C(C3=NC(C)=CN=C3)C=C2Cl)=CC4=CN=C(NCCC5CCN(C)CC5)N=C4N1CC |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Description
FRAX-1036 is a potent and selective inhibitor with biochemical potency (Ki) of 23.3 nM and 72.4 nM against PAK1 and PAK2.
Targets
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. And treatment of OVCAR-3 cells with FRAX-1036 results in upregulation of p53 and p21, while down-regulating cyclin B1.
In vivo
Treatment with Frax1036 results in slower KT21 tumor growth and is unlikely to have significant blood brain barrier permeability in mice.
References
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