Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0003528
PMID 7990108
  Assay Used Kinase assay and HaCaT keratinocyte proliferation assay
  Experimently ValidatedYes
  EGFR (IC50) > 100000 nM
  HER2 (IC50)  -
  HER4 (IC50)  -
  Mutant L858R (IC50)  -
  Mutant T790M (IC50)  -
  Double Mutant (IC50)  -
  Average ERBB2 and ERBB1 (IC50) -
  Inhibition EGFR (%) -
  Inhibitory Concentration -
  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 novel antiproliferative agents aerived from Lavendustin A
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1A431- 213000 ±28000 nM -- -- ----
2B16F1- 269000 nM -- -- ----
3HaCaT- 40 nM -- -- ----
4HeLa- 470000 ±212100 nM -- -- ----
5K562- 217500 ±31800 nM -- -- ----
6KB- 191500 ±12000 nM -- -- ----
7L1210- 415000 ± 7100 nM -- -- ----
8LOVO- 185000 ±7100 nM -- -- ----
9MCF-7- 19000 ± 8500 nM -- -- ----
10MDA-MB-231- 427500 ±130800 nM -- -- ----
11MDA-MB-468- 46500 ±14100 nM -- -- ----
12P388- 337500 ± 123700 nM -- -- ----
13SCL-1- 383000 nM -- -- ----
14SKBR3- 31000 ±1400 nM -- -- ----
15u937- 320000 nM -- -- ----

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

Inhibitor Binding
  EGFR-
  HER2-
  HER4-