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JH-IX-179 | JH-IX-179 : Inhibitor of FLT3
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
FLT3 (Mutant:FLT3-ITD, FLT3-N841I, and FLT3-D835V)
    • IC50:4.28 nM
    • IC50:10.22 nM
    • IC50:2 nM
    • IC50:11 nM
    Inhibitor
    up to 100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    KinomeScan binding analysis against a near-comprehensive panel of 456 kinases at a concentration of ...

    Potency
    Cellular
    In Vitro

    FLT3 (Mutant:FLT3-ITD, FLT3-N841I, and FLT3-D835V)

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acsmedchemlett.5b00498

    Chemical Information

    Molecular Formula C26H24N6O
    SMILEs CN(C)CCCn1cc(-c2ccc3c(c2)-c2[nH]c4cc(-c5cn[nH]c5)ccc4c2C3=O)cn1
    InChI InChI=1S/C26H24N6O/c1-31(2)8-3-9-32-15-19(14-29-32)16-4-6-20-22(10-16)25-24(26(20)33)21-7-5-17(11-23(21)30-25)18-12-27-28-13-18/h4-7,10-15,30H,3,8-9H2,1-2H3,(H,27,28)
    Molecular weight 436.20 Da
    AlogP 0.0
    HBond acceptors 7
    HBond donors 2
    Atoms 57

    Vendors

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    Expert Reviews

    by SERP+
    (on 17 Jun 2024 )
    Cellular Use Rating
    This is a potent FLT3 inhibitor. For some off-targets, especially CIT and FLT3-wt as well as other FLT-3 mutations, no IC50 values were determined, even though the compound showed significant inhibition...
    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