Epidermal Growth Factor Receptor Inhibitor Database


Experimental Information
  
Enzymatic Activity
Molecule Id EGIN0000649
PMID 17062696
  Assay Used Recombinant protein Kinases, aswell as in cell proliferation assays
  Experimently ValidatedYes
  EGFR (IC50)  22 /L nM
  HER2 (IC50)  32 nM
  HER4 (IC50)  190 nM
  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 Preclinical Antitumor Activity of BMS-599626 Kinase Inhibitor That Inhibits HER1/HER2 Homodimer and Heterodimer Signaling.
  Extra -

Cellular Activity
S.No. Cell Line Desp. IC50 IC80 ED50 GI50 GI90 EC50 Kd Inhibition (%) Inhibitory Conc.
1A2780-> 10000 nM -- -- ----
2AU565- 630 nM -- -- ----
3BT474- 310 nM -- -- ----
4GEO- 900 nM -- -- ----
5HCC1419- 750 nM -- -- ----
6HCC1954- 340 nM -- -- ----
7HCC202- 940 nM -- -- ----
8KPL-4- 380 nM -- -- ----
9MDA-MB-175- 840 nM -- -- ----
10MRC5-> 10000 nM -- -- ----
11N87- 450 nM -- -- ----
12PC9- 340 nM -- -- ----
13Sal2- 240 nM -- -- ----
14ZR-75-30- 510 nM -- -- ----

Activity against Receptor
  EGFR Yes
  HER2Yes
  HER4Yes
  Wild typeYes
  Mutant-

Inhibitor Binding
  EGFR-
  HER2-
  HER4-