Name: CP-673451
Price: 320.00 USD

- Overview
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    Background
    
    CP-673451 is a potent inhibitor of PDGFR with IC50 value of 10nM and 1nM for PDGFR-α and PDGFR-β, respectively [1].CP-673451 is an ATP-competitive inhibitor and is investigated to treat for cancer. It is highly selective against PDGFR-α and PDGFR-β over a variety of other kinases such as VEGFR-1, VEGFR-2, Lck, TIE-2 and EGFR. In PAE-β cells, CP-673451 inhibits PDGFR-β with IC50 value of 6.4nM. CP-673451 also inhibits c-kit with IC50 value of 1.1μM in H526 cells. In rat C6 glioblastoma xenograft models, a single oral dose of 50mg/kg CP-673451 reduces > 50% phosphorylation of PDGFR-β for 4 hours. In addition, CP-673451 is found to inhibit PDGF-BB-induced angiogenesis in a sponge angiogenesis model. Furthermore, CP-673451 inhibits the tumor growth in Colo205, LS174T, H460, and U87MG xenograft models. It also reduces the microvessel density of Colo205 xenografts [1].
    
    [1] Roberts W G, Whalen P M, Soderstrom E, et al. Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer research, 2005, 65(3): 957-966.
- Properties
  - Alternative Name
    
    1-[2-[5-(2-methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-amine
    
    CAS Number
    
    343787-29-1
    
    Molecular Formula
    
    C24H27N5O2
    
    Molecular Weight
    
    417.52
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; ≥2.39 mg/mL in EtOH with gentle warming and ultrasonic; ≥20.9 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

CP-673451

CP-673451

Background

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