Name: FRAX597
Price: 284.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    FRAX597 is a small-molecule inhibitor of the group 1 p21-activated kinases (PAKs) with IC50 values of 8nM, 13nM and 19nM, respectively for PAK1, PAK2 and PAK3 [1]. The PAKs family includes two sub groups: 1 and 2. These kinases take participate in the growth of various types of cancers. FRAX597 is developed to be an inhibitor of group 1 PAKs from the initial hits of a high throughput screen. It is an ATP-competitive inhibitor of PAK 1-3. To group 2 PAKs, FRAX597 shows minimal inhibitory activity. The inhibition mechanism of FRAX597 is that it binds PAK by targeting the ATP binding site and competes with ATP. FRAX597 is reported to suppress cell proliferation by arresting cell cycle in G1 without impacting cell viability in Schwann cells. In vivo assay also demonstrates FRAX597 can suppress tumor growth in an orthotopic model of NF2. This effect on the cells has been proved to be mediated through the inhibition of the group I PAKs [1].
    
    [1] Silvia Licciulli, Jasna Maksimoska, Chun Zhou, Scott Troutman, Smitha Kota, Qin Liu, Sergio Duron, David Campbell, Jonathan Chernoff, Jeffery Field, Ronen Marmorstein and Joseph L. Kissil. FRAX597, a small molecule inhibitor of the p21-activated kinases, inhibits schwannomas tumorigenesis of NF2-associated. J. Biol. Chem. 2013, August.
- Properties
  - Alternative Name
    
    6-[2-chloro-4-(1,3-thiazol-5-yl)phenyl]-8-ethyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrido[2,3-d]pyrimidin-7-one
    
    CAS Number
    
    1286739-19-2
    
    Molecular Formula
    
    C29H28ClN7OS
    
    Molecular Weight
    
    558.1
    
    Appearance
    
    A solid
    
    Purity
    
    98.76%
    
    Solubility
    
    ≥27.9 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. White SM, Avantaggiati ML, et al. "YAP/TAZ Inhibition Induces Metabolic and Signaling Rewiring Resulting in Targetable Vulnerabilities in NF2-Deficient Tumor Cells." Dev Cell. 2019 May 6;49(3):425-443.e9. PMID:31063758
    2. Nuche-Berenguer B, Ramos-álvarez I, Jensen RT. "The p21-activated kinase, PAK2, is important in the activation of numerous pancreatic acinar cell signaling cascades and in the onset of early pancreatitis events." Biochim Biophys Acta. 2016 Jun;1862(6):1122-36. PMID:26912410

FRAX597

FRAX597

Background

We Also Recommend

MK-4827 hydrochloride

MK-4827 tosylate

Pimobendan hydrochloride