Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000006
PMID 21306821
  Assay Used Enzymatic and Cell growth inhibition assay
  Experimently ValidatedYes
  EGFR (IC50)  -
  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 Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor,alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1AGSKRAS mt 1930 ± 180 nM -- -- ----
2N87HER2 amp 130 ± 2 nM -- -- ----
3SNU1KRAS mt 1610 ± 30 nM -- -- ----
4SNU16FGFR2 amp 1840 ± 90 nM -- -- ----
5SNU216HER2 amp 150 ± 8 nM -- -- ----
6SNU484– 990 ± 660 nM -- -- ----
7SNU5MET amp 3930 ± 740 nM -- -- ----
8SNU601KRAS mt 1220 ± 640 nM -- -- ----
9SNU620– 2130 ± 30 nM -- -- ----
10SNU638MET amp 4510 ± 480 nM -- -- ----
11SNU668KRAS mt 2320 ± 10 nM -- -- ----
12SNU719– 4950 ± 640 nM -- -- ----

Activity against Receptor
  EGFR Yes
  HER2Yes
  HER4Yes
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFR-
  HER2-
  HER4-