Atirmociclib | Atirmociclib : Inhibitor of CDK4, CDK6
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
In Vivo
Control Compounds
Vendors

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK4
  • Ki:0.7 nM
  • IC50:36 nM
  • IC50:47 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Biochemical assays with 265 recombinant kinases in in vitro enzymatic assays (CARNA) by 1 μM atirmoc ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
A set of 25 cell lines were tested with Atirmociclib and the following were found sensitive to treat ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
in a biochemical Assay using recombinant CDK6- cyclin D3, CDK6 activity was 23 nM
In Cell Selectivity Assessment
Potency Assay Off-Target:
IC50 of 2881 nM, assessing phosphorylation of RB1 at serine 807/811 from CDK4 independent human pri ...

Potency
Cellular
In Vitro

CDK4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.ccell.2025.02.006

Orthogonal Probes def

PALBOCICLIB
ABEMACICLIB

Chemical Information

Molecular Formula C22H27ClFN5O3
InChI InChI=1S/C22H27ClFN5O3/c1-11(2)29-16-8-12(7-14(24)19(16)27-20(29)22(3,4)31)18-13(23)9-25-21(28-18)26-15-5-6-32-10-17(15)30/h7-9,11,15,17,30-31H,5-6,10H2,1-4H3,(H,25,26,28)/t15-,17-/m1/s1
Molecular weight 463.18 Da
AlogP 0.0
HBond acceptors 8
HBond donors 3
Atoms 59

References

Cross References

canSARChEMBLBindingDB

Expert Reviews


(on 16 May 2025 )
Cellular Use Rating
Atirmociclib is a CDK4-preferring inhibitor currently in clinical development by Pfizer, following the CDK4/6 unselective compound Palbociclib. Given its development stage, this molecule has been robustly...
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