Name: FRAX1036
Price: 286.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: N/AFRAX1036 is a p21-activated kinase I (PAK1) inhibitor.Breast cancer is a clinically and molecularly heterogeneous disease and plenty of genetic and epigenetic studies of breast tumors has revealed novel putative driver genes, such as p21-activated kinase (PAK)1. As a serine/threonine kinase downstream of small GTP-binding proteins including Rac1 and Cdc42, PAK1 is an critical component of growth factor signaling networks and cellular functions important to tumorigenesis.In vitro: Previous study demonstrated that the administration of docetaxel with either FRAX1036 or PAK1 small interfering RNA oligonucleotides was able to alter signaling to cytoskeletal-associated proteins dramatically, such as stathmin, and also able to induce microtubule disorganization and cellular apoptosis. In addition, the live-cell imaging data showed that the duration of mitotic arrest mediated by docetaxel could be significantly reduced by the treatment of FRAX1036, which was associated with increased kinetics of apoptosis [1]. In vivo: In previous animal study, the untreated mice bearing KT21 transplants showed ventricular invasion, whereas Ben-Men grew at the injection site. Efficacy results found that the treatment with Frax1036 could lead to a slower tumor growth, with reduction in body mass index (BMI) signals of 37% when compared to vehicle cohort [2]. Clinical trial: Up to now, FRAX1036 is still in the preclinical development stage.
    
    [1] Ong CC et al. Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res.2015 Apr 23;17:59.
    [2] Chow HY et al. Group I Paks as therapeutic targets in NF2-deficient meningioma. Oncotarget.2015 Feb 10;6(4):1981-94.
- Properties
  - Alternative Name
    
    6-(2-chloro-4-(6-methylpyrazin-2-yl)phenyl)-8-ethyl-2-((2-(1-methylpiperidin-4-yl)ethyl)amino)pyrido[2,3-d]pyrimidin-7(8H)-one
    
    CAS Number
    
    1432908-05-8
    
    Molecular Formula
    
    C28H32ClN7O
    
    Molecular Weight
    
    518.05
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    98.00%
    
    Solubility
    
    Soluble in DMSO
    
    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

We Also Recommend

GSK591

$265

MS023

$242

Tubercidin

$183

Tubercidin

$280

FRAX1036

FRAX1036

Background

We Also Recommend

GSK591

MS023

Tubercidin

Tubercidin