CX-6258

- Overview
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    Background
    
    Pim kinases (Provirus Integration site for Moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. This family of kinases is composed of three different isoforms (Pim-1, Pim-2, and Pim-3). The simultaneous inhibition of Pim-1, Pim-2, and Pim-3 kinases is emerging as a promising strategy for anticancer drug development. CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.
    In vitro: CX-6258 exhibited in vitro synergy with chemotherapeutics. The antiproliferative activity of CX-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. CX-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].
    In vivo: CX-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia MV-4-11, and prostate adenocarcinoma PC3. The drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI. In addition, CX-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where Pim kinases had been shown to play an important role [1].
    Clinical trial: No clinical data are available
- Properties
  - Alternative Name
    
    CX6258;CX 6258; (E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one
    
    CAS Number
    
    1202916-90-2
    
    Molecular Formula
    
    C26H24ClN3O3
    
    Molecular Weight
    
    461.94
    
    Appearance
    
    A solid
    
    Purity
    
    98.28%
    
    Solubility
    
    insoluble in EtOH; ≥11.15 mg/mL in DMSO; ≥2.575 mg/mL in H2O with gentle warming
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CX-6258

Background

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