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CP-673451 | CP-673451 : ATP competitive inhibitor of PDGFRB
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PDGFRB
  • IC50:1 nM
  • IC50:1 nM
  • IC50:6.4 nM
PDGFRA
  • IC50:10 nM
    100 nM

    Selectivity

    In Vitro Selectivity Assessment

    Potency: IC50 - KIT 252 nM, VEGFR1 450 nM, VEGFR2 450 nM

    Potency Assay Off-Target:
    CP673451 was tested at 100 nM in Kinase Profiler assay in vitro, and was 1,000-10,000-fold selective ...
    In Cell Selectivity Assessment

    Potency: IC50 - KIT 1 uM

    Potency Assay Off-Target:
    Inhibition of substrate phosphorylation

    Potency
    Cellular
    In Vitro

    PDGFRB

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1158/0008-5472.957.65.3

    PDGFRA

    Mode of Action: ATP Competitive

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1158/0008-5472.957.65.3

    In Vivo Validations

    Mouse
    Dose: 10-100 mg/kg
    Route of delivery: Oral
    Plasma half life: 2-3 hr
    Cmax: 5.5 ng/mL @ 33 mg/Kg
    Organ of interest (O): xenograft
    Target engagement assay: Ex vivo ELISA to assess inhibition of substrate phosphorylation

    Reference: --

    Chemical Information

    Molecular Formula C24H27N5O2
    SMILEs COCCOc1ccc2c(c1)ncn2-c1ccc2cccc(N3CCC(N)CC3)c2n1
    InChI InChI=1S/C24H27N5O2/c1-30-13-14-31-19-6-7-21-20(15-19)26-16-29(21)23-8-5-17-3-2-4-22(24(17)27-23)28-11-9-18(25)10-12-28/h2-8,15-16,18H,9-14,25H2,1H3
    Molecular weight 417.22 Da
    AlogP 3.5264000000000015
    HBond acceptors 7
    HBond donors 2
    Atoms 58

    References

    Publications

    Cross References

    ChEMBL BindingDB PDB PubChem canSAR

    Vendors

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    Expert Reviews

    by SERP
    (on 18 Aug 2016)
    Cellular Use Rating
    Chemical Neighbourhood for QSAR: 18 molecules similar (>0.80) to CP-673451 with in vitro affinities for PDGFRbeta were found in public repositories (e.g., ChEMBL). On-Target links to toxicities:...
    by SERP
    (on 2 Nov 2016)
    Cellular Use Rating
    In Model Organisms
    The limited public information on this compound does not provide high confidence in its utility as a probe to evaluate PDGFR biology. The probe has been reported to enzyme potency in 1-10 nM range with...
    by SERP
    (on 15 Jun 2017)
    Cellular Use Rating
    In Model Organisms
    The published data for CP-673451 indicates that it is a highly potent and selective inhibitor of PDGFR relative to other anti-antiogenic receptors, including VEGFR, TIE-2 and c-KIT, though the panel...
    Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria