Epidermal Growth Factor Receptor Inhibitor Database Experimental Information Page

Epidermal Growth Factor Receptor Inhibitor Database

Experimental Information

Enzymatic Activity
Molecule Id	EGIN0000005
PMID	12384534
Assay Used	Substrate inhibition assay with EGFR prepared from the human vulval squamous carcinoma cell line A431, MTT assay was used to measure cell growth
Experimently Validated	Yes
EGFR (IC₅₀)	33 nM
HER2 (IC₅₀)	3700 ± 10000 nM
HER4 (IC₅₀)	-
Mutant L858R (IC₅₀)	-
Mutant T790M (IC₅₀)	-
Double Mutant (IC₅₀)	-
Average ERBB2 and ERBB1 (IC₅₀)	-
Inhibition EGFR (%)	-
Inhibitory Concentration	-
Inhibition HER2 (%)	-
Inhibitory Concentration	-
K_i (EGFR)	-
K_i (HER2)	-
K_i (HER4)	-
K_d (EGFR)	-
K_d (L858R)	-
K_d (T790M)	-
K_d (L858R/T790M)	-
K_d (Other mutation)	-
Note	ZD1839 is a potent EGFR-TKI in vitro. It is a competitive inhibitor of ATP and therefore binds at the ATP site on EGFR, it demonstrates remarkable selectivity for EGFR compared with other RTKs that share sequence homology in the ATP binding domain.The paper describes the ZD1839 (Iressa)as an Orally Active Inhibitor of Epidermal Growth Factor Signaling with Potential for Cancer Therapy
Extra	0.027 µM [ EGFR (baculovirus lysate) ]

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Cellular Activity

S.No.

Cell Line

Desp.

IC₅₀

IC₈₀

ED₅₀

GI₅₀

GI₉₀

EC₅₀

K_d

Inhibition (%)

Inhibitory Conc.

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