Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0001016
PMID 17184594
  Assay Used Tyrosine Kinase assays by ELISA, Cell growth inhibition assay by sulforhodamine B(SRB),Cell growth inhibition assay by MTT
  Experimently ValidatedYes
  EGFR (IC50)  -
  HER2 (IC50)  -
  HER4 (IC50)  -
  Mutant L858R (IC50)  -
  Mutant T790M (IC50)  -
  Double Mutant (IC50)  -
  Average ERBB2 and ERBB1 (IC50) -
  Inhibition EGFR (%) 35.50%
  Inhibitory Concentration 10 µM/L
  Inhibition HER2 (%) -
  Inhibitory Concentration -
  Ki (EGFR)-
  Ki (HER2)-
  Ki (HER4)-
  Kd (EGFR)-
  Kd (L858R)-
  Kd (T790M)-
  Kd (L858R/T790M)-
  Kd (Other mutation)-
  Note The paper describes the 3,5-substituted indolin-2-one derivatives as antitumor agents
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1A431- - -- -- --7.80%10 µmol/L
2A549- - -- -- --31.80%10 µmol/L
3ADPKD- 45900 nM -- -- ----
4MDA-MB-468- - -- -- --1.90%10 µmol/L

Activity against Receptor
  EGFR Yes
  HER2-
  HER4-
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFR-
  HER2-
  HER4-