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INX-315 | INX-315 : Inhibitor of CDK2
RATINGS:
Cellular Use: (2 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
CDK2
  • IC50:0.6 nM
  • IC50:2.5 nM
  • IC50:2.3 nM
  • IC50:71 nM
Inhibitor
100 nM
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
The intracellular IC50 (NanoBRET) for INX-315 and CDK1/cyclin B1 was 374 nM while the IC50 for CDK9/ ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within family (IC50): CDK1/B1 30 nM, CDK2/cyclin E1 0.6 nM, CDK2/cyclin A2 2.5 nM, CDK3/ ...

Potency
Cellular
In Vitro

CDK2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/2159-8290.CD-23-0954

Orthogonal Probes def

CANSAR4002324

Chemical Information

Molecular Formula C19H21N7O3S
SMILEs NS(=O)(=O)c1ccc(Nc2ncc3cc4n(c3n2)C2(CCCCC2)C(=O)NN4)cc1
InChI InChI=1S/C19H21N7O3S/c20-30(28,29)14-6-4-13(5-7-14)22-18-21-11-12-10-15-24-25-17(27)19(8-2-1-3-9-19)26(15)16(12)23-18/h4-7,10-11,24H,1-3,8-9H2,(H,25,27)(H2,20,28,29)(H,21,22,23)
Molecular weight 427.14 Da
AlogP 0.0
HBond acceptors 10
HBond donors 5
Atoms 51

References

Publications

Cross References

canSARBindingDB

Expert Reviews

by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
Based on the data, CSF1R should be considered as off-target. This probe, unfortunately does not have an inactive control compound, but PF-07104091 can be used as orthogonal probe for CDK2, with good off-target...
by SERP
(on 1 Jul 2024 )
Cellular Use Rating
While this probe is touted as highly selective for CDK2, it will depend on the setting and the biology, e.g. the corresponding cyclin partner, whether selectivity can be considered significant enough to...
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