Name: ON123300
Price: 265.00 USD

- Overview
  - Please contact us at for specific academic pricing.
    
    Background
    
    IC50: 3.9, 5, 26, 26, 9.2 and 11 nM for CDK4, Ark5, PDGFRβ, FGFR1, RET, and Fyn, respectively.ON123300 is a multi-targeted kinase inhibitor.The signaling hyperactivation of RTK is most commonly caused by EGFR mutation/amplification or PDGFR amplification/overexpression. FGFR1signaling also occurs in GBM exhibiting FGFR1 kinase domain gain-of-function mutations.In vitro: In previous study, when Z138C and Granta 519 cells were treated with ON123300, it was found that ON123300 was efficient to inhibit the phosphorylation of Rb family proteins. Moreover, ON123300 was able to inhibit the phosphorylation of proteins that were involved in the PI3K/AKT pathway. In addition, ON123300-treated cells similarly arrested at lower concentrations, however, higher concentrations could lead to the apoptosis induction [1]. In vivo: Previous animal in vivo study showed that mouse xenograft had a strong inhibition of MCL tumor growth in ON123300-treated animals. Moreover, the treatment with ON123300 to ibrutinib-sensitive and -resistant patient-derived MCLs was able to trigger apoptosis and inhibition of both Rb and PI3K/AKT pathways, indicating that ON123300 could be an effective drug in the treatment of MCL, such as ibrutinib-resistant forms of the disease [1]. Clinical trial: Up to now, ON12300 is still in the preclinical development stage.
- Properties
  - Alternative Name
    
    8-cyclopentyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidine-6-carbonitrile
    
    CAS Number
    
    1357470-29-1
    
    Molecular Formula
    
    C24H27N7O
    
    Molecular Weight
    
    429.52
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥21.5 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

ON123300

ON123300

Background

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