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AC710 | Inhibitor of CSF1R, FLT3, KIT, PDGFRB, PDGFRA
RATINGS:
Cellular Use: (2 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
CSF1R
  • Kd:0.5 nM
  • IC50:10.5 nM
FLT3
  • Kd:0.6 nM
  • IC50:2 nM
KIT
  • Kd:1 nM
  • IC50:1.2 nM
PDGFRB
  • Kd:1 nM
  • IC50:7.7 nM
PDGFRA
  • Kd:1.3 nM
    Inhibitor
    100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    Selectivity determined against a panel of 386 unique kinases @ 1 uM. Kinase Binding Affinities (< 1, ...
    In Cell Selectivity Assessment
    Selectivity Assessment Description:
    pFLT3 IC50 2 in MV4-11, pKIT IC50 1.2 in H526, pPDGFRβ IC50 7.7 in MG-63 cells. Clean cytochrome P45 ...

    Potency
    Cellular
    In Vitro

    CSF1R

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/ml300214g

    FLT3

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/ml300214g

    KIT

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/ml300214g

    PDGFRB

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/ml300214g

    PDGFRA

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/ml300214g

    In Vivo Validations

    Mouse
    Dose: 3, 10, 30 mg/Kg
    Route of delivery: Intraperitoneal
    Systemic clearance: 14 mL/min/Kg

    DOI Reference: 10.1021/ml300214g

    Chemical Information

    Molecular Formula C31H42N6O4
    SMILEs CCN1C(C)(C)CC(Oc2ccc(C(=O)Nc3ccc(NC(=O)Nc4cc(C(C)(C)C)on4)cc3)nc2)CC1(C)C
    InChI InChI=1S/C31H42N6O4/c1-9-37-30(5,6)17-23(18-31(37,7)8)40-22-14-15-24(32-19-22)27(38)33-20-10-12-21(13-11-20)34-28(39)35-26-16-25(41-36-26)29(2,3)4/h10-16,19,23H,9,17-18H2,1-8H3,(H,33,38)(H2,34,35,36,39)
    Molecular weight 562.33 Da
    AlogP 6.6837
    HBond acceptors 10
    HBond donors 3
    Atoms 83

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

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    Expert Reviews

    by SERP
    (on 19 Mar 2021 )
    Cellular Use Rating
    In Model Organisms
    The probe binds with selectivity for kinases of the PDGFR family. The selectivity of the inhibitor for this family of kinases is based on affinity (Kd) studies against a panel of 386 kinases. The ability...
    by SERP
    (on 10 Apr 2021 )
    Cellular Use Rating
    In Model Organisms
    Potent PDGFR family inhibitor (cell “close to target assay” IC50 values are 1.2, 2, 7.7 and 10.5 nM for KIT, FLT3, PDGFRβ and CSF1R respectively in H526,MV411,MG-63, and M-NFS-60 cells, respectively...
    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