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PALBOCICLIB | PALBOCICLIB : ATP competitive inhibitor of CDK4, CDK6
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CDK4
  • IC 50:11 nM
  • IC 50:66 nM
CDK6
  • IC 50:16 nM
  • IC 50:66 nM
ATP competitive
3 nM - 3 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC 50 - DUSP1A 2000 nM, MAPK9 8000 nM

Selectivity Assessment Description:
>10 uM for all other kinases tested (CDK1, CDK2, CDK5, EGFR, FGFR, PDGFR, LCK, VEGFR, AMPK, CHEK1, C ...

Potency
Cellular
In Vitro

CDK4

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

PMID Reference: 15542782

CDK6

Mode of Action: ATP competitive

Structure-Activity-Relationship data available? Yes

PMID Reference: 15542782

Chemical Information

Molecular Formula C24H29N7O2
SMILEs CC(=O)c1c(C)c2cnc(Nc3ccc(N4CCNCC4)cn3)nc2n(C2CCCC2)c1=O
InChI InChI=1S/C24H29N7O2/c1-15-19-14-27-24(28-20-8-7-18(13-26-20)30-11-9-25-10-12-30)29-22(19)31(17-5-3-4-6-17)23(33)21(15)16(2)32/h7-8,13-14,17,25H,3-6,9-12H2,1-2H3,(H,26,27,28,29)
Molecular weight 447.24 Da
AlogP 0.0
HBond acceptors 9
HBond donors 2
Atoms 62

Expert Reviews

by SERP
(on 16 May 2016 )
Cellular Use Rating
In Model Organisms
Additional kinase selectivity data can be found on the MRC website (http://www.kinase-screen.mrc.ac.uk/screening-compounds/348821). Cellular target- engagement studies would strengthen support for using...
by SERP
(on 22 Jun 2016 )
Cellular Use Rating
In Model Organisms
PD0332991 leads to complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg.
by SERP
(on 4 Jun 2017 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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