PALBOCICLIB

ATP-competitive inhibitor of CDK4, CDK6

Structure

SERP Rating

In Cells

(3 ratings)

In Model Organisms

(3 ratings)

note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars.

Information

CDK4
CDK6

ATP-competitive inhibitor

PMID - 15542782

Probe Availability:

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

Off-Target Selectivity Assesments

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

Probe Selectivity in Vitro:

>10 uM for all other kinases tested (CDK1, CDK2, CDK5, EGFR, FGFR, PDGFR, LCK, VEGFR, AMPK, CHEK1, CSNK1, CSNK2, SRC, CSK, GSK3B, JUN, ERK2, MAPKAPK2, MAPK1, MAPK8, RPS6KB1, PDPK1, PHK, PRKACA, AKT1, PRKC, MAPKAPK5, ROCK1, MAPK14, MAP2K6, MAP2K4)

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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 )