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Lapatinib | Inhibitor of EGFR, ERBB2
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
EGFR
  • IC 50:10.2 nM
  • IC 50:170 nM
ERBB2
  • IC 50:9.8 nM
  • IC 50:80 nM
Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - 367 nM ERBB4

Potency Assay Off-Target:
In vitro kinase activity
Selectivity Assessment Description:
enzyme inhibitory activity reveal, C-Src IC50 3500 and IC50 > 10000 nM for c-Raf-1, MEK. ERK, ...

Potency
Cellular
In Vitro

EGFR

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

PMID Reference: 12467226

ERBB2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

PMID Reference: 12467226

In Vivo Validations

Mouse
Dose: 30-100 mg/Kg
Route of delivery: Oral

PMID Reference: 12467226

Orthogonal Probes def

Canertinib
Afatinib
SJF1528

Chemical Information

Molecular Formula C29H26ClFN4O4S
SMILEs CS(=O)(=O)CCNCc1ccc(-c2ccc3ncnc(Nc4ccc(OCc5cccc(F)c5)c(Cl)c4)c3c2)o1
InChI InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35)
Molecular weight 580.13 Da
AlogP 6.1391
HBond acceptors 8
HBond donors 2
Atoms 66

References

Publications

Cross References

canSARChEMBLBindingDBPDBe (Protein Data Bank Europe)

Vendors

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Expert Reviews

No SERP comments found for Lapatinib

Probe Lapatinib is in the process of SERP review.

Please continue to check back for new reviews and commentary.