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FMF-02-063-1 | FMF-02-063-1 : Inhibitor of PIK3CD and PIK3CG
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (0 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
PIK3CD
  • IC50:2.1 nM
  • IC50:1.4 µM, 1.3 µM, 0.62 µM, 1.0 µM, 0.35 µM
PIK3CG
  • IC50:6.5 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    activity detected by KINOMEscan® at 1 μ M compound concentration: PI3K-α IC50 =55 nM +/- 16 nM PI3K- ...
    Selectivity Assessment Description:
    activity detected by KINOMEscan®

    Potency
    Cellular
    In Vitro

    PIK3CD

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acsmedchemlett.6b00209

    PIK3CG

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acsmedchemlett.6b00209

    Chemical Information

    Molecular Formula C25H28N6O4S
    SMILEs Cc1ccc2c(c1)C(=O)N(C)c1cnc(Nc3cccc(S(=O)(=O)N4CCC(O)CC4)c3)nc1N2C
    InChI InChI=1S/C25H28N6O4S/c1-16-7-8-21-20(13-16)24(33)30(3)22-15-26-25(28-23(22)29(21)2)27-17-5-4-6-19(14-17)36(34,35)31-11-9-18(32)10-12-31/h4-8,13-15,18,32H,9-12H2,1-3H3,(H,26,27,28)
    Molecular weight 508.19 Da
    AlogP 3.03192
    HBond acceptors 10
    HBond donors 2
    Atoms 64

    Vendors

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    Expert Reviews

    by SERP+
    (on 22 Mar 2023)
    Cellular Use Rating
    The compound showed poor selectivity to PI3K alpha (IC50 value of 55 ± 16 nM). A cellular target engagement assay is not available.
    by SERP+
    (on 23 Sept 2024)
    Cellular Use Rating
    The compound possesses good in vitro and in cell potency. There is however insufficient selectivity for PI3K-delta and PI3K-gamma over PI3K-alpha. Whilst IC50 values show ~20-fold difference (PI3K-alpha:...
    by SERP
    (on 23 Oct 2024)
    Cellular Use Rating
    (The reviewer did not leave any public comments)
    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