CP-724714

Inhibitor of ERBB2

Structure

Information

Protein target names: ERBB2

Mechanism of action: Inhibitor

Recommended in-cell concentration:
50 nM - 10 uM

In Vitro Validations

Uniprot ID: P04626
Target Class:
Target SubClass: RTK
Potency: IC50
Potency Value: 3 nM
Potency Assay: In vitro kinase assay with intracellular domain
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Receptor tyrosine-protein kinase erbB-2, NGL, NEU, ...

DOI Reference: 10.1158/0008-5472.CAN-06-3559

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

Comments:

CP-724714 is available commercially through several vendors, and the scientific community has been using the agent largely as a cellular probe for selective and potent inhibition of HER2/ERBB2. It has an IC50 of 10 nM, and is >640-fold selective against EGFR, InsR, IRG-1R, PDGFR, VEGFR2, ABL, SRC, c-MET, etc. in cell-free assays. The published information regarding the use of CP-724714 in various cell lines and in animals makes this a valuable probe for cellular assays.

(last updated: 17 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

If I were going to use this compound in my studies, I would also likely include Mubritinib (TAK-165), which is a potent inhibitor of HER2/ErbB2 with IC50 of 6 nM in BT-474 cells and shows no activity against EGFR, FGFR, PDGFR, JAK1, SEC or BLK in BT-474 cell lines. 

(last updated: 18 Oct 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

Comments:

CP-724714 is a potent inhibitor of ERBB2 kinase in both cell-free (IC50=10 nM) and cellular (IC50=32 nM) assays with good selectivity over EGFR kinase (>500-fold) and other representative kinases (>1000-fold). Published data supports the use of CP-724714 in both cellular and mouse models at reasonable concentrations and doses. A 25 mg/kg oral dose in mouse is rapidly absorbed and achieved plasma levels of 12.5 ug/mL at 30 min. 

(last updated: 22 Jan 2017 )

SERP Ratings

Comments:

CP-724714 is a selective, cell-permeable chemical probe for ERBB2, with minimal collateral engagement to other tyrosine kinases. It has 10 nM potency with solid cellular and biophysical characterization. It has been validated in a number of cancer cell lineages, supporting its general use as a chemical probe for cellular applications. Cellular studies should be performed with >50 nM CP-724714.

(last updated: 23 Jan 2017 )