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GNE-2861

Chemical Structure : GNE-2861

CAS No.: 1394121-05-1

GNE-2861 (GNE2861)

Catalog No.: PC-62720Not For Human Use, Lab Use Only.

GNE-2861 is a potent, selective group II PAK (PAK4/5/6) inhibitor with IC50 of 7.5/126/36 nM, respectively, shows selectivity over group I PAKs (IC50=5.42/0.97/>10 uM for PAK1/2/3).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GNE-2861 is a potent, selective group II PAK (PAK4/5/6) inhibitor with IC50 of 7.5/126/36 nM, respectively.
GNE-2861 shows selectivity over group I PAKs (IC50=5.42/0.97/>10 uM for PAK1/2/3).
GNE-2861 decreases tumor cell migration and invasion in triple-negative breast cancer cell lines, perturbs estrogen receptor alpha signaling and restores tamoxifen-sensitivity in breast cancer cells.

Physicochemical Properties

M.Wt 406.49
Formula C22H26N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(2-(1-(2-aminopyrimidin-4-yl)-2-((2-methoxyethyl)amino)-1H-1,3-benzodiazol-6-yl)ethynyl)cyclohexan-1-ol

References

1. Staben ST, et al. J Med Chem. 2014 Feb 13;57(3):1033-45.

2. Zhuang T, et al. Oncotarget. 2015 Dec 22;6(41):43853-68.

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