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DCLK1-IN-1 | DCLK1-IN-1 : Inhibitor of DCLK1, DCLK2
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
DCLK1
  • Kd:109 nM
  • IC50:9.5 nM
  • IC50:57.2 nM
  • IC50:279 nM
DCLK2
  • IC50:31 nM
  • IC50:103 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    KINOMEscan profiling at a concentration of 1 μM t across a panel of 489 human kinases. DCLK1-IN-1 ex ...
    In Cell Selectivity Assessment
    Potency Assay Off-Target:
    Kinativ: DCLK1-IN-1 significantly inhibited DCLK1, and weakly inhibited ERK5, in PATU-8988T cell lys ...

    Potency
    Cellular
    In Vitro

    DCLK1

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/s41589-020-0506-0

    DCLK2

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1038/s41589-020-0506-0

    In Vivo Validations

    Mouse
    Dose: 10 mg/Kg
    Route of delivery: Oral
    Cmax: 1014.69 ng/mL
    Tmax: 1.00 h
    Area Under the Curve:: 5506 h/ng/ml
    Bioavailability: 81%

    DOI Reference: 10.1038/s41589-020-0506-0

    Dose: 2 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 2.09 h
    Systemic clearance: 26.26 ml/min/Kg
    Area Under the Curve:: 1269.45 h/ng/mL
    Volume of Distribution at Steady-State: 3.27 L/Kg

    DOI Reference: 10.1038/s41589-020-0506-0

    Negative Control Compounds

    DCLK1-NEG
    Notes: DCLK1-NEG displayed at least 100-fold lower activity against DCLK1

    Chemical Information

    Molecular Formula C26H28F3N7O2
    SMILEs COc1cc(N2CCN(C)CC2)ccc1Nc1ncc2c(n1)N(C)c1ccccc1C(=O)N2CC(F)(F)F
    InChI InChI=1S/C26H28F3N7O2/c1-33-10-12-35(13-11-33)17-8-9-19(22(14-17)38-3)31-25-30-15-21-23(32-25)34(2)20-7-5-4-6-18(20)24(37)36(21)16-26(27,28)29/h4-9,14-15H,10-13,16H2,1-3H3,(H,30,31,32)
    Molecular weight 527.23 Da
    AlogP 0.0
    HBond acceptors 9
    HBond donors 1
    Atoms 66

    References

    Publications

    Cross References

    canSARChEMBLBindingDBPDBPubMedPubMed

    Vendors

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    Expert Reviews

    by SERP
    (on 21 Feb 2023 )
    Cellular Use Rating
    In Model Organisms
    DCLK1-IN-1 is high quality chemical probe suitable for in vitro as well as in vivo experiments to study DCLK1 and DCLK2 protein kinases. Its high kinome-wide selectivity was confirmed by testing at 1 uM...
    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