PD0332991

ATP-competitive inhibitor of CDK4, CDK6

Structure

Information

Protein target names: CDK4, CDK6

Mechanism of action: ATP-competitive inhibitor

Primary References:

In Vitro Validations

Uniprot ID: P11802
Target Class: Kinase
Target SubClass: CMGC
Potency: IC 50
Potency Value: 11 nM
Potency Assay: Inhibition of substrate-GST fusion phosphorylation
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Cyclin-dependent kinase 4, CDK4, CDK4_HUMAN, PSK-J ...

PMID Reference: 15542782

In Cell Validations

In Vivo Data

No in Vivo Validations

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

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 this as a probe and would further link the target to the phenotype.

(last updated: 16 May 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

PD0332991 leads to complete tumor stasis in a MDA-MB-435 xenograft at 150 mg/kg.

(last updated: 22 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 4 Jun 2017 )