Lapatinib

Inhibitor of EGFR, ERBB2

Probe Lapatinib is in the process of SERP review.

Please continue to check back for new reviews and commentary.

Probe Availability:

Uniprot ID: P00533

Target Class: Kinase

Target SubClass: RTK

Potency: IC 50

Potency Value: 10.2 nM

Potency Assay: In vitro kinase assay using intracellular kinase domain

PDB ID for probe-target interaction (3D structure): 1XKK

Structure-activity relationship: yes

Target aliases:

Epidermal growth factor receptor, HER1, ERBB1, ERB ...

PMID Reference: 12467226

Potency end-point : IC50 367 nM ERBB4

Potency assay (off target): In vitro kinase activity

Probe Selectivity in Vitro:

enzyme inhibitory activity reveal, C-Src IC50 3500 and IC50 > 10000 nM for c-Raf-1, MEK. ERK, c-Fms, CDK1, CDK2, p38, Tie-2, VEGFR-2

No SERP comments found for Lapatinib