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CP-724714 | Inhibitor of ERBB2
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

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Targets Biochemical/Biophysical Potency Cellular Potency
ERBB2
  • IC50:3 nM
  • IC50:32 nM
50 nM - 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - EGFR 6400 nM

Potency Assay Off-Target:
In vitro kinase assay on intracellular domain >1,000-fold selective for ERBB2 over IGF1R, PDGFRbeta ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
Selective for ERBB2 over EGFR in cells

Potency
Cellular
In Vitro

ERBB2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

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

In Vivo Validations

Mouse
Dose: 2.5 mg/kg
Route of delivery: Oral
Organ of interest (O): xenograft
Target engagement assay: Indirect: inhibition of protein substrate phosphorylation detected by ex vivo ELISA in xenograft tumor tissue

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

Chemical Information

Molecular Formula C27H27N5O3
SMILEs COCC(=O)NC/C=C/c1ccc2ncnc(Nc3ccc(Oc4ccc(C)nc4)c(C)c3)c2c1
InChI InChI=1S/C27H27N5O3/c1-18-13-21(8-11-25(18)35-22-9-6-19(2)29-15-22)32-27-23-14-20(7-10-24(23)30-17-31-27)5-4-12-28-26(33)16-34-3/h4-11,13-15,17H,12,16H2,1-3H3,(H,28,33)(H,30,31,32)/b5-4+
Molecular weight 469.21 Da
AlogP 4.953340000000003
HBond acceptors 8
HBond donors 2
Atoms 62

Expert Reviews

by SERP
(on 17 Jun 2016)
Cellular Use Rating
In Model Organisms
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...
by SERP
(on 18 Oct 2016)
Cellular Use Rating
In Model Organisms
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...
by SERP
(on 22 Jan 2017)
Cellular Use Rating
In Model Organisms
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....
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