Chemical Probes logo
BI-1347 | BI-1347 : Inhibitor of CDK8 and CDK19
RATINGS:
Cellular Use: (0 reviews)

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

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK8
  • Kd:0.77 nM
  • EC50:5 nM
  • IC50:3 nM
  • EC50:10 nM
CDK19
  • IC50:1.7 nM
    Inhibitor
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Invitrogen® panel: 369 kinases screened @ 10 µM Selected IC50 measured @ Invitrogen®: CDK8 IC50 = 1. ...

    Potency
    Cellular
    In Vitro

    CDK8

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acsmedchemlett.9b00480

    CDK19

    Mode of Action: Inhibitor

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1158/1535-7163.MCT-19-0789

    In Vivo Validations

    Mouse
    Dose: 1 mg/Kg IV, 10 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 15% QH
    Bioavailability: 93%
    Volume of Distribution at Steady-State: 0.5 L/Kg

    Reference: --

    Rat
    Dose: 3 mg/Kg IV, 10 mg/Kg PO
    Route of delivery: Intravenous, Oral
    Systemic clearance: 14% QH
    Bioavailability: 69%
    Volume of Distribution at Steady-State: 0.4 L/Kg

    Reference: --

    Negative Control Compounds

    BI-1374
    Notes: Inhibition of pSTAT S727 in NK-92 cells IC50> 10000 nM
    SMILES: CN(C)C(CN(N=C1)C=C1C(C=C2)=CC=C2C3=NN=C4C=CC=CN43)=O

    Orthogonal Probes def

    CCT251545

    Chemical Information

    Molecular Formula C22H20N4O
    SMILEs CN(C)C(=O)Cn1cc(-c2ccc(-c3cncc4ccccc34)cc2)cn1
    InChI InChI=1S/C22H20N4O/c1-25(2)22(27)15-26-14-19(12-24-26)16-7-9-17(10-8-16)21-13-23-11-18-5-3-4-6-20(18)21/h3-14H,15H2,1-2H3
    Molecular weight 356.16 Da
    AlogP 3.853500000000002
    HBond acceptors 5
    HBond donors --
    Atoms 47

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    No SERP comments found for BI-1347

    Probe BI-1347 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.