Chemical Probes logo
SR-4835 | SR-4835 : ATP competitive inhibitor of CDK12, CDK13
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
CDK12
  • Kd:98 nM
  • IC50:99.0 ± 10.5 nM
  • EC50:105.5 ± 5.50 nM
  • EC50:15-25 nM
CDK13
  • Kd:4.9 nM
    ATP competitive
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    SR-4835 was highly selective toward CDK12 and CDK13 when tested in a panel of over 450 kinases at 10 ...

    Potency
    Cellular
    In Vitro

    CDK12

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.ccell.2019.09.004

    CDK13

    Mode of Action: ATP competitive

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.ccell.2019.09.004

    In Vivo Validations

    Mouse
    Dose: 20 mg/Kg
    Route of delivery: Oral
    Plasma half life: 3.95 h
    Systemic clearance: 29.52 mL/min/kg
    Cmax: 1301 ng/mL
    Tmax: 2.67 h
    Area Under the Curve:: 23.27 uM*h

    DOI Reference: 10.1016/j.ccell.2019.09.004

    Chemical Information

    Molecular Formula C21H20Cl2N10O
    SMILEs Cn1cc(-n2cnc3c(NCc4nc5cc(Cl)c(Cl)cc5[nH]4)nc(N4CCOCC4)nc32)cn1
    InChI InChI=1S/C21H20Cl2N10O/c1-31-10-12(8-26-31)33-11-25-18-19(29-21(30-20(18)33)32-2-4-34-5-3-32)24-9-17-27-15-6-13(22)14(23)7-16(15)28-17/h6-8,10-11H,2-5,9H2,1H3,(H,27,28)(H,24,29,30)
    Molecular weight 498.12 Da
    AlogP 0.0
    HBond acceptors 11
    HBond donors 2
    Atoms 54

    Vendors

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

    Expert Reviews

    No SERP comments found for SR-4835

    Probe SR-4835 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.