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AZ13705339
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C33H36FN7O3S
- MW: 629.75
Description
AZ13705339 is a highly potent, ATP-competitive, and selective PAK1 and PAK2 inhibitor with IC50 values of 0.33 and 6 nM for PAK1 and PAK2, respectively. It showed greater than 7,500-fold selectivity over isoform PAK4 and exhibits robust selectivity over a panel of more than 100 non-group I kinases. It serves as a valuable in vitro probe compound in oncology research.
AZ13705339 enables mechanistic studies of PAK1/2 signaling and target validation across biochemical, cellular, and translational disease models.
Key Features
- PAK1 inhibitor for interrogation of PAK1 biology
- IC50 values of 0.33 for PAK1 and 6 nM for PAK2
- Modulates PAK1-dependent signaling or biological activity
- AZ13705339 is a potent and selective PAK1 inhibitor (IC50 value of 0.33 nM)
Applications
- PAK pharmacology and target-validation studies
- PAK pathway and signaling assays
- Disease-relevant cellular and translational model systems
- Kinase signaling, phosphorylation and pathway-inhibition assays
More Information
| Parent CAS No. | 2016806-57-6 |
|---|---|
| Chemical Name | 2-(((2-(3-(Ethylsulfonyl)-4-(4-methylpiperazin-1-yl)phenylamino)-5-fluoropyrimidin-4-yl)(5-(hydroxymethyl)-2-methylphenyl)amino)methyl)benzonitrile |
| SMILES | C1(N2CCN(C)CC2)C=CC(NC2N=CC(F)=C(N(CC3C(C#N)=CC=CC=3)C3C=C(CO)C=CC=3C)N=2)=CC=1S(CC)(=O)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C33H36FN7O3S/c1-4-45(43,44)31-18-27(11-12-29(31)40-15-13-39(3)14-16-40)37-33-36-20-28(34)32(38-33)41(21-26-8-6-5-7-25(26)19-35)30-17-24(22-42)10-9-23(30)2/h5-12,17-18,20,42H,4,13-16,21-22H2,1-3H3,(H,36,37,38) |
| InChiKey | WPFLVPJXKWCRQK-UHFFFAOYSA-N |
| CID | 129909860 |
| Short Description | PAK1 inhibitor |
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