Cat. No.: HY-10261

Afatinib

(Synonyms: BIBW 2992)

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Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC₅₀ values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer.

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Pureté: 99.92%
CAS No.: 850140-72-6
Formule: C₂₄H₂₅ClFN₅O₃
Masse moléculaire:485.94

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Afatinib Chemical Structure

CAS No.: 850140-72-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (107)
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Activité biologique

Description

IC₅₀ & Target^[1]

EGFR^L858R

0.4 nM (IC₅₀)

EGFR

0.5 nM (IC₅₀)

EGFR^L858R/T790M

10 nM (IC₅₀)

HER2

14 nM (IC₅₀)

HER3

Voir tous les produits spécifiques à Isoform EGFR :

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform p38 MAPK :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.023 nM Compound: 6, BIBW2992	Antiproliferative activity against human A431 cells after 72 hrs by SRB assay Antiproliferative activity against human A431 cells after 72 hrs by SRB assay	[PMID: 24183742]
A-431	IC₅₀	0.02 μM Compound: 5, BIBW2992	Antiproliferative activity against human A431 cells assessed as growth inhibition after 72 hrs by SRB assay Antiproliferative activity against human A431 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 24565969]
A-431	IC₅₀	0.9 μM Compound: Afatinib	Antiproliferative activity against human A431 cells after 48 hrs by Celltiter-Glo assay Antiproliferative activity against human A431 cells after 48 hrs by Celltiter-Glo assay	[PMID: 25409491]
A-431	EC₅₀	0.6 μM Compound: Afatinib	Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
A-431	EC₅₀	0.2 μM Compound: Afatinib	Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A-431	IC₅₀	10.21 nM Compound: Afatinib	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by CCK8 assay Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by CCK8 assay	[PMID: 30600209]
A-431	IC₅₀	1.4 μM Compound: Afatinib	Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human A431 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
A-431	EC₅₀	0.535 μM Compound: Afatinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A-431	GI₅₀	0.594 μM Compound: Afatinib	Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
A549	IC₅₀	1.811 μM Compound: Afatinib	Cytotoxicity against human A549 cells after 48 hrs by MTT assay Cytotoxicity against human A549 cells after 48 hrs by MTT assay	[PMID: 24900830]
A549	IC₅₀	0.05 μM Compound: BIBW-2992	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26906472]
A549	IC₅₀	1.4 μM Compound: BIBW-2992	Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28428040]
A549	EC₅₀	1.49 μM Compound: Afatinib	Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
A549	IC₅₀	3766 nM Compound: Afatinib	Antiproliferative activity against human A549 cells harboring wild-type EGFR after 72 hrs by EZ-Cytox assay Antiproliferative activity against human A549 cells harboring wild-type EGFR after 72 hrs by EZ-Cytox assay	[PMID: 30554954]
A549	IC₅₀	5 μM Compound: Afatinib	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
A549	IC₅₀	6.32 μM Compound: Afatinib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 31648877]
A549	IC₅₀	1.2 μM Compound: Afatinib	Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35728507]
A549	IC₅₀	5.4 μM Compound: Afatinib	Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 37141440]
A549	IC₅₀	1.24 μM Compound: Afatinib	Antiproliferative activity against human A549 cells overexpressing c-Met and EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells overexpressing c-Met and EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37984296]
BaF3	IC₅₀	>1 μM Compound: 6	Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay	[PMID: 26258521]
BaF3	IC₅₀	381.3 nM Compound: Afatinib	Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Cytotoxicity against mouse BaF3 cells expressing IL-3 assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
BaF3	EC₅₀	0.097 μM Compound: Afatinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	GI₅₀	0.015 μM Compound: Afatinib	Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay	[PMID: 35486541]
BaF3	IC₅₀	1.58 nM Compound: Afatinib	Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR A763-Y764 ins FQEA mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR A763-Y764 ins FQEA mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	1.61 nM Compound: Afatinib	Antiproliferative activity against mouse BAF3 cells harboring HER2-P780-Y781 ins GSP mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2-P780-Y781 ins GSP mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	37.8 nM Compound: Afatinib	Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR D770-N771 ins NPG mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring FL-EGFR D770-N771 ins NPG mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	9.9 nM Compound: Afatinib	Antiproliferative activity against mouse BAF3 cells harboring HER2-A775-G776 ins YVMA mutant after 72 hrs by celltiter-Glo luminescence assay Antiproliferative activity against mouse BAF3 cells harboring HER2-A775-G776 ins YVMA mutant after 72 hrs by celltiter-Glo luminescence assay	[PMID: 36804726]
BaF3	IC₅₀	3.8 nM Compound: Afatinib	Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring wild type EGFR incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	40 nM Compound: Afatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR-D770-N771insNPG mutant incubated for 3 days by Cell Titer-Glo assay	[PMID: 37669428]
BaF3	IC₅₀	19.96 nM Compound: Afatinib	Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771insSVD by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring EGFR D770_N771insSVD by CellTiter-Glo assay	[PMID: 38518121]
BXPC-3	EC₅₀	>1000 nM Compound: Afatinib	Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 27010810]
Caco-2	IC₅₀	7.7 μM Compound: Afatinib	Antiproliferative activity against human Caco2 cells by MTT assay Antiproliferative activity against human Caco2 cells by MTT assay	[PMID: 30216848]
Calu-3	GI₅₀	2.77 nM Compound: cpd A	Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human Calu-3 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
CL97	IC₅₀	0.1 μM Compound: Afatinib	Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
HCC827	IC₅₀	8 nM Compound: 9, BIBW-2992	Antiproliferative activity against human HCC827 cells after 96 hrs by MTS assay Antiproliferative activity against human HCC827 cells after 96 hrs by MTS assay	[PMID: 20550212]
HCC827	EC₅₀	<0.014 μM Compound: Afatinib	Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
HCC827	IC₅₀	0.4376 nM Compound: Afatinib	Antiproliferative activity against human HCC827 cells harboring EGFR L858R mutant after 72 hrs by CCK8 assay Antiproliferative activity against human HCC827 cells harboring EGFR L858R mutant after 72 hrs by CCK8 assay	[PMID: 30600209]
HCC827	CC₅₀	14 nM Compound: Afatinib	Cytotoxicity in human HCC827 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human HCC827 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]
HCC827	IC₅₀	0.23 nM Compound: Afatinib	Antiproliferative activity against human HCC827 cells by CellTiter-Glo assay Antiproliferative activity against human HCC827 cells by CellTiter-Glo assay	[PMID: 38518121]
HCT-116	IC₅₀	11.4 μM Compound: Afatinib	Antiproliferative activity against human HCT116 cells by MTT assay Antiproliferative activity against human HCT116 cells by MTT assay	[PMID: 30216848]
HCT-116	IC₅₀	5.3 μg/mL Compound: Afatinib	Cytotoxicity against human HCT-116 cells Cytotoxicity against human HCT-116 cells	[PMID: 34655985]
HeLa	IC₅₀	6.81 μM Compound: BIBW-2992	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 26906472]
HeLa	IC₅₀	6.2 μM Compound: Afatinib	Antiproliferative activity against human HeLa cells by MTT assay Antiproliferative activity against human HeLa cells by MTT assay	[PMID: 30216848]
HeLa	IC₅₀	6.39 μM Compound: Afatinib	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 31648877]
HepG2	IC₅₀	1.33 μM Compound: BIBW-2992	Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28428040]
HepG2	IC₅₀	5.3 μg/mL Compound: Afatinib	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 34655985]
L02	CC₅₀	25.3 μM Compound: Afatinib	Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 31648877]
LoVo	IC₅₀	0.012 μM Compound: 3	Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay	[PMID: 23930994]
LoVo	IC₅₀	15 nM Compound: 11; BIBW-2992	Growth inhibition of human LoVo cells harboring wild type EGFR Growth inhibition of human LoVo cells harboring wild type EGFR	[PMID: 32432477]
MCF7	IC₅₀	5.83 μM Compound: BIBW-2992	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26906472]
MCF7	IC₅₀	2.63 μM Compound: BIBW-2992	Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28428040]
MCF7	IC₅₀	7.1 μM Compound: Afatinib	Antiproliferative activity against human MCF7 cells by MTT assay Antiproliferative activity against human MCF7 cells by MTT assay	[PMID: 30216848]
MCF7	IC₅₀	7.62 μM Compound: Afatinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 31648877]
MDA-MB-231	EC₅₀	>1000 nM Compound: Afatinib	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27010810]
MDA-MB-231	IC₅₀	7.5 μM Compound: Afatinib	Antiproliferative activity against human MDA231 cells by MTT assay Antiproliferative activity against human MDA231 cells by MTT assay	[PMID: 30216848]
NCI-H1975	IC₅₀	0.023 μM Compound: 3	Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T790M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
NCI-H1975	IC₅₀	0.148 μM Compound: 6, BIBW2992	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant after 72 hrs by SRB assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant after 72 hrs by SRB assay	[PMID: 24183742]
NCI-H1975	IC₅₀	0.15 μM Compound: 5, BIBW2992	Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as growth inhibition after 72 hrs by SRB assay Antiproliferative activity against gefitinib-resistant human NCI-H1975 cells assessed as growth inhibition after 72 hrs by SRB assay	[PMID: 24565969]
NCI-H1975	IC₅₀	0.392 μM Compound: Afatinib	Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay Cytotoxicity against human NCI-H1975 cells after 48 hrs by MTT assay	[PMID: 24900830]
NCI-H1975	IC₅₀	0.9 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells after 48 hrs by Celltiter-Glo assay Antiproliferative activity against human NCI-H1975 cells after 48 hrs by Celltiter-Glo assay	[PMID: 25409491]
NCI-H1975	GI₅₀	107.1 nM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition	[PMID: 26310890]
NCI-H1975	IC₅₀	0.9 μM Compound: 39	Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as decrease in cell viability after 48 hrs by WST assay Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant assessed as decrease in cell viability after 48 hrs by WST assay	[PMID: 26882288]
NCI-H1975	EC₅₀	116 nM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay	[PMID: 27010810]
NCI-H1975	IC₅₀	1.97 μM Compound: Afatinib	Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo assay Cytotoxicity against human NCI-H1975 cells assessed as decrease in cell viability after 72 hrs by CellTiter-Glo assay	[PMID: 28274675]
NCI-H1975	EC₅₀	0.7 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay	[PMID: 28603991]
NCI-H1975	EC₅₀	0.6 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay	[PMID: 28853575]
NCI-H1975	IC₅₀	131 nM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by EZ-Cytox assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by EZ-Cytox assay	[PMID: 30554954]
NCI-H1975	IC₅₀	96.07 nM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant after 72 hrs by CCK8 assay	[PMID: 30600209]
NCI-H1975	IC₅₀	1 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
NCI-H1975	CC₅₀	224 nM Compound: Afatinib	Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method Cytotoxicity in human NCI-H1975 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method	[PMID: 31560541]
NCI-H1975	IC₅₀	5.55 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 31648877]
NCI-H1975	IC₅₀	22 nM Compound: 11; BIBW-2992	Growth inhibition of human NCI-H1975 cells harboring EGFR L858R/T790M double mutant Growth inhibition of human NCI-H1975 cells harboring EGFR L858R/T790M double mutant	[PMID: 32432477]
NCI-H1975	IC₅₀	12.68 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition by MTT assay	[PMID: 32739648]
NCI-H1975	IC₅₀	0.92 μM Compound: Afatinib	Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]
NCI-H1975	IC₅₀	0.37 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay	[PMID: 35178185]
NCI-H1975	IC₅₀	93 nM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant assessed as inhibition of EGFR phosphorylation Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M mutant assessed as inhibition of EGFR phosphorylation	[PMID: 35728507]
NCI-H1975	IC₅₀	0.9 μM Compound: Afatinib	Antiproliferative activity against human NCI-H1975 cells overexpressing c-Met and EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells overexpressing c-Met and EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37984296]
NCI-H1993	IC₅₀	>12.5 μM Compound: Afatinib	Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay Cytotoxicity against human NCI-H1993 cells after 48 hrs by MTT assay	[PMID: 24900830]
NCI-H358	GI₅₀	1 nM Compound: cpd A	Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
NCI-H460	IC₅₀	6.14 μM Compound: Afatinib	Antiproliferative activity against human H460 cells assessed as reduction in cell viability after 24 hrs by MTT assay Antiproliferative activity against human H460 cells assessed as reduction in cell viability after 24 hrs by MTT assay	[PMID: 31648877]
NIH3T3	IC₅₀	3.605 μM Compound: Afatinib	Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay Cytotoxicity against mouse NIH/3T3 cells after 48 hrs by MTT assay	[PMID: 24900830]
NSCLC	IC₅₀	0.5 nM Compound: BIBW-2992	Cytotoxicity against human NSCLC cells Cytotoxicity against human NSCLC cells	[PMID: 26906472]
PC-3	IC₅₀	4.1 μM Compound: BIBW-2992	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 26906472]
PC-3	IC₅₀	3.96 μM Compound: BIBW-2992	Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 72 hrs by MTT assay	[PMID: 28428040]
PC-9	IC₅₀	0.00057 μM Compound: 3	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
PC-9	IC₅₀	0.57 nM Compound: 3	Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
PC-9	IC₅₀	0.638 nM Compound: Afatinib	Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Anticancer activity against human PC-9 cells harboring del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
PC-9	IC₅₀	1130 nM Compound: Afatinib	Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Anticancer activity against human PC-9 cells harboring C797S/T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
PC-9	IC₅₀	61.94 nM Compound: Afatinib	Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay Anticancer activity against human PC-9 cells harboring T790M/del19 mutant assessed as inhibition of cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 28287083]
PC-9	IC₅₀	0.1 nM Compound: Afatinib	Antiproliferative activity against human PC9 cells harboring EGFR exon-19 del mutant after 72 hrs by EZ-Cytox assay Antiproliferative activity against human PC9 cells harboring EGFR exon-19 del mutant after 72 hrs by EZ-Cytox assay	[PMID: 30554954]
PC-9	IC₅₀	<0.01 μM Compound: Afatinib	Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31446247]
PC-9	IC₅₀	0.3 nM Compound: Afatinib	Antiproliferative activity against human PC-9 cells Antiproliferative activity against human PC-9 cells	[PMID: 33429247]
PC-9	GI₅₀	0.37 nM Compound: cpd A	Antiproliferative activity against human PC-9 cells expressing EGFR E746/A750 deletion mutant assessed as reduction in cell viability after 72 hrs by CCK-8 assay Antiproliferative activity against human PC-9 cells expressing EGFR E746/A750 deletion mutant assessed as reduction in cell viability after 72 hrs by CCK-8 assay	[PMID: 35364239]
PC-9	IC₅₀	5 nM Compound: 2	Cytotoxicity against human PC-9 cells harboring EGFR mutant assessed as inhibition of cell growth Cytotoxicity against human PC-9 cells harboring EGFR mutant assessed as inhibition of cell growth	[PMID: 36410591]
PC-9	IC₅₀	1.08 μM Compound: Afatinib	Antiproliferative activity against human PC-9 cells overexpressing c-Met and EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-9 cells overexpressing c-Met and EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37984296]
Sf21	IC₅₀	14 nM Compound: Afatinib	Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (696 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (696 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate	[PMID: 30554954]
Sf21	IC₅₀	37 nM Compound: Afatinib	Inhibition of human C-terminal His6-tagged ERBB2 (676 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate Inhibition of human C-terminal His6-tagged ERBB2 (676 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate	[PMID: 30554954]
Sf21	IC₅₀	9 nM Compound: Afatinib	Inhibition of human N-terminal GST-tagged EGFR kinase domain (696 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate Inhibition of human N-terminal GST-tagged EGFR kinase domain (696 to end residues) expressed in baculovirus infected sf21 cells using poly(Glu, Tyr) 4:1 as substrate	[PMID: 30554954]
Sf9	IC₅₀	0.5 nM Compound: 39	Inhibition of human wild type GST-tagged EGFR kinase domain expressed in insect Sf9 cells using pEY (4:1)/biotinylated pEY as substrate after 30 mins by ELISA Inhibition of human wild type GST-tagged EGFR kinase domain expressed in insect Sf9 cells using pEY (4:1)/biotinylated pEY as substrate after 30 mins by ELISA	[PMID: 26882288]
Sf9	IC₅₀	15.4 nM Compound: Afatinib	Inhibition of C-terminal His-tagged N-terminal GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells after 30 mins in presence of gamma-[32p-ATP] binding assay Inhibition of C-terminal His-tagged N-terminal GST-tagged human EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells after 30 mins in presence of gamma-[32p-ATP] binding assay	[PMID: 31648877]
SK-BR-3	IC₅₀	1.2 nM Compound: Afatinib	Antiproliferative activity against HER2-dependant human SKBR3 cells after 72 hrs by EZ-Cytox assay Antiproliferative activity against HER2-dependant human SKBR3 cells after 72 hrs by EZ-Cytox assay	[PMID: 30554954]
SW-620	IC₅₀	2.13 μM Compound: Afatinib	Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay Antiproliferation activity against EGFR-negative human SW620 cells assessed as reduction in cell viability incubated incubated for 48 hrs by MTT assay	[PMID: 32912431]

In Vitro

Afatinib (100 nM) sufficiently prevents heregulin-stimulated HER3 phosphorylation^[1].
Afatinib (0-10000 nM) effectively inhibits anchorage-independent proliferation of NIH-3T3 cells ectopically expressing EGFR mutants, and inhibits cell proliferation of H1666, H3255, and NCI 1975 cells^[1].
Afatinib (48-72 h)shows growth inhibition in HKESC-1, HKESC-2, SLMT-1 and EC-1 cells^[2].
Afatinib (0-1 μM, 24-48 h) inhibits AKT and MAPK pathways, and inhibits EGFR and AKT phosphorylation in ESCC cell lines^[2].
Afatinib (0-1 μM, 16-48 h) induces G0/G1 cell cycle arrest in HKESC-2 and EC-1^[2].
Afatinib (0-1 μM, 24-48 h) effectively induces apoptotic cell death in HKESC-2 and EC-1^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

NIH-3T3 cells, H1666, H3255, and NCI 1975 cells
Concentration:

0, 1, 10, 100, 1000, 10000 nM
Incubation Time:
Result:

Effectively inhibited anchorage-independent proliferation of NIH-3T3 cells ectopically expressing EGFR mutants. Showed inhibition of anchorage independent cell proliferation of various lung cancer cell lines (H1666, H3255, and NCI 1975 cells), with IC₅₀ values of 60 nM, 0.7 nM and 99 nM, respectively.

Cell Viability Assay^[2]

Cell Line:

HKESC-1, HKESC-2, SLMT-1 and EC-1 cell lines
Concentration:
Incubation Time:

48 and 72 hours
Result:

Observed over 95% of growth inhibition. The respective IC₅₀ concentrations at 48 hours (HKESC-1=0.078 μM, HKESC-2=0.115 μM, KYSE510=3.182 μM, SLMT-1=4.625 μM and EC-1=1.489 μM) and 72 hours (HKESC-1=0.002 μM, HKESC-2=0.002 μM, KYSE510=1.090 μM, SLMT-1=1.161 μM and EC-1=0.109 μM) were all in lower micro-molar range.

Western Blot Analysis^[2]

Cell Line:

HKESC-2 cells and EC-1 cells
Concentration:

0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
Incubation Time:

24 and 48 hours
Result:

Reduced the phosphorylation of EGFR and the endogenous expression level of HER2 receptors in ESCC cells. Suppressed AKT phosphorylation in a dose and time dependent manner. Significantly reduced the phosphorylation level of the downstream effectors of the AKT-mTOR axis especially in HKESC-2 cells. Inhibited the two major downstream pathways of the ErbB/HER axis, namely, AKT and MAPK pathways in ESCC cell lines.

Cell Cycle Analysis^[2]

Cell Line:

HKESC-2 cells and EC-1 cells
Concentration:

0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
Incubation Time:

16, 24, and 48 hours
Result:

Induced G0/G1 cell cycle arrest in both tested ESCC cell lines in a time and dose dependent manner. In HKESC-2 cells, the percentage of cells in G0/G1 phase was increased from 38.2% to 68.1% at 0.01 μM of afatinib and to 74.7% at 0.1 μM of afatinib, from 24 hours (82.4% G0/G1 arrest at 0.01 μM and 86.2% at 0.1 μM) to 48 hours (from 74.7% to 88.2% for 0.01 μM and 91.0% for 0.1 μM). In EC-1 cells, the percentage of cells arrested in the G0/G1 phase was increased from 59.1% to 66.6% and 72.2% at 24 and 48 hours respectively.

Apoptosis Analysis^[2]

Cell Line:

HKESC-2 cells and EC-1 cells
Concentration:

0, 0.01, and 0.1 μM (HKESC-2 cells), 0, 0.1 and 1 μM (EC-1 cells)
Incubation Time:

24 and 48 hours
Result:

Effectively induced cell death by triggering apoptotic mechanisms in ESCC cell lines. Showed a stronger expression level of cleaved Poly (ADP-ribose) polymerase (PARP) in these cell lines.

In Vivo

Afatinib (0-20 mg/kg, Orally, daily for 25 days) shows dramatic tumor regression and downregulation of EGFR, HER2, HER3 and AKT phosphorylation^[1].
Afatinib (15 mg/kg, Orally, in a schedule of 5 days on plus 2 days off, for two weeks) strongly inhibits the growth of HKESC-2 tumor^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Athymic NMRI-nu/nu female mice (21–31 g, five to six-week-old, transgenic murine lung cancer model and xenograft models)^[1]
Dosage:

15 mg/kg, 20 mg/kg
Administration:

Orally, daily for 25 days
Result:

Resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2% in a standard xenograft model of the epidermoid carcinoma cell line A431, and downregulation of EGFR and AKT phosphorylation. Induced regression of large tumors in this HER2-driven model, effectively controlled xenograft tumor formation by the NCIH1975 cell line, expressing EGFR L858R/T790M, with a T/C value of 12% for doses of 20 mg/kg. Induced more than 50% percent tumor reduction after a 4-week treatment period. Downregulated EGFR, HER2 and HER3 phosphorylation.

Animal Model:

Six weeks old female athymic nude mice (nu/nu) (16-20 g)^[2]
Dosage:

15 mg/kg
Administration:

Oral gavage in a schedule of 5 days on plus 2 days off, for two weeks
Result:

Strongly inhibited the growth of HKESC-2 tumor. Average tumor sizes of vehicle and treatment at end point are 348 ± 24 mm³ and 108 ± 36 mm³ respectively.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 850140-72-6
Appearance Solid
Masse moléculaire 485.94
Formule C₂₄H₂₅ClFN₅O₃
Color White to yellow
SMILES

O=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[C@H]4CCOC4)/C=C/CN(C)C
Synonyms

BIBW 2992
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (107)

All WBFlow CytometryIn Vivo Efficacy StudyIHCOthersCell Proliferation/Viability AssayRT-PCR

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Journal Impact Factor

Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171

Afatinib purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

Immunoblot analysis of cell lines (K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines) treated for 15 h with AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM).

Afatinib purchased from MedChemExpress. Usage Cited in: Nature. 2026 Jan;649(8098):1032-1041. [Abstract]

Luminescent reporter assay of K562 HER2WT or HER2C805S Nluc-3xFLAG reporter cell lines treated for 15 h with the indicated compounds (AV-412 (HY-10346; 2.5 µM), neratinib (HY-32721; 10 µM), afatinib (HY-10261; 10 µM), WZ4002 (HY-12026; 10 µM)) shown as normalized luminescence per genetic construct (two-way ANOVA, Sidak corrected) (n = 3).
Cancer Cell

2026 May 21:S1535-6108(26)00220-5. PMID: 42167227
Cancer Cell

Anti-tumor efficacy of HRS-4642 and its potential combination with proteasome inhibition in KRAS G12D-mutant cancer. [Abstract]

2024 Jul 8;42(7):1286-1300.e8. PMID: 38942026
Cancer Cell

KMT2D deficiency drives lung squamous cell carcinoma and hypersensitivity to RTK-RAS inhibition. [Abstract]

2023 Jan 9;41(1):88-105.e8. PMID: 36525973

Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2023 Jan 9;41(1):88-105.e8. [Abstract]

Cell viability assays of Kmt2d KO LUSC cell lines, Kmt2d WT LUSC cell lines, and LUAD (KP) cell line treated with afatinib for 72h. Data presented as mean ± SD (n = 3). The calculated IC50 values of afatinib is shown below.
J Hematol Oncol

SMARCA4 controls state plasticity in small cell lung cancer through regulation of neuroendocrine transcription factors and REST splicing. [Abstract]

2024 Jul 30;17(1):58. PMID: 39080761
Cancer Discov

Tumor-Intrinsic Kinome Landscape of Pancreatic Cancer Reveals New Therapeutic Approaches. [Abstract]

2025 Feb 7;15(2):346-362. PMID: 39632628
Nat Genet

Loss of Kmt2c or Kmt2d primes urothelium for tumorigenesis and redistributes KMT2A-menin to bivalent promoters. [Abstract]

2025 Jan;57(1):165-179. PMID: 39806204

Afatinib purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jan;57(1):165-179. [Abstract]

Afatinib (10 mg/kg/day; daily, 5 days per week by oral gavage) decreased the intensity of EGFR phosphorylation (pY845) in NOD-SCID mice.

Afatinib purchased from MedChemExpress. Usage Cited in: Nat Genet. 2025 Jan;57(1):165-179. [Abstract]

Afatinib (10 mg/kg/day; daily, 5 days per week by oral gavage) reduced the number of Ki-67-positive proliferating cells in NOD-SCID mice.
Nat Cell Biol

Growth factor-triggered de-sialylation controls glycolipid-lectin-driven endocytosis. [Abstract]

2025 Mar;27(3):449-463. PMID: 39984654
Cancer Res

C-terminal Truncation and Fusion Partner Determine Oncogenicity of FGFR3. [Abstract]

2025 Dec 29. PMID: 41460723
Cancer Res

NF1 Loss Promotes EGFR Activation and Confers Sensitivity to EGFR Inhibition in NF1 Mutant Melanoma. [Abstract]

2025 Jun 10:10.1158/0008-5472.CAN-24-3904. PMID: 40494652

Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 10:10.1158/0008-5472.CAN-24-3904. [Abstract]

Growth curves of NF1^Mut melanoma STCs treated with 0.1, 0.5, 1, 5, or 10 μM Afatinib.

Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Res. 2025 Jun 10:10.1158/0008-5472.CAN-24-3904. [Abstract]

Growth curves of NF1^Mut melanoma STCs treated with 0.1, 0.5, 1, 5, or 10 μM Afatinib.
Mol Cell

Amplified dosage of the NKX2-1 lineage transcription factor controls its oncogenic role in lung adenocarcinoma. [Abstract]

2025 Mar 21:S1097-2765(25)00194-7. PMID: 40139189
Cancer Res

Targeting c-Myc to Overcome Acquired Resistance of EGFR Mutant NSCLC Cells to the Third-Generation EGFR Tyrosine Kinase Inhibitor, Osimertinib. [Abstract]

2021 Sep 15;81(18):4822-4834. PMID: 34289988
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Nat Commun

An alternative EGFR activation by patient-derived R252C mutation promotes cancer progression. [Abstract]

2026 Jan 21;17(1):1902. PMID: 41565660
Nat Commun

Fructose intake driven glycolysis-ROS-EGFR axis specifically promotes the generation and pathogenicity of Th17 cells. [Abstract]

2025 Nov 23;16(1):11115. PMID: 41276507
Nat Commun

PPARα-mediated lipid metabolism reprogramming supports anti-EGFR therapy resistance in head and neck squamous cell carcinoma. [Abstract]

2025 Feb 1;16(1):1237. PMID: 39890801

Afatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]

mRNA expression for CPT1A in cetuximab-sensitive (-S) and -resistant (-R) FaDu cells upon treatment with gefitinib, afatinib, selumetinib or buparlisib (2 µM each, for 24 h) (N = 3, n = 3).

Afatinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1237. [Abstract]

mRNA expression for CPT1A in cetuximab-sensitive (-S) and -resistant (-R) SC263 cells upon treatment with gefitinib, afatinib, selumetinib or buparlisib (2 µM each, for 24 h) (N = 3, n = 3).
Nat Commun

AURKB as a target in non-small cell lung cancer with acquired resistance to anti-EGFR therapy. [Abstract]

2019 Apr 18;10(1):1812 PMID: 31000705
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Chem Eng J

2024 May 15, 488, 150822.
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
J Exp Clin Cancer Res

Pyrotinib targeted EGFR/GRP78 mediated cell apoptosis in high EGFR gene copy number gastric cancer. [Abstract]

2025 Aug 19;44(1):245. PMID: 40830980
J Exp Clin Cancer Res

Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. [Abstract]

2024 Nov 20;43(1):308. PMID: 39567998
J Exp Clin Cancer Res

The potential of swine pseudorabies virus attenuated vaccine for oncolytic therapy against malignant tumors. [Abstract]

2023 Oct 27;42(1):284. PMID: 37891570
Redox Biol

C-terminal interleukin 1 alpha (IL-1α) overexpression drives EMT and a vulnerability to ferroptosis in HNSCC. [Abstract]

2026 Jun:93:104172. PMID: 42013543
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 2:102053. PMID: 40187357
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Pharmacol Res

Chelidonine selectively inhibits the growth of gefitinib-resistant non-small cell lung cancer cells through the EGFR-AMPK pathway. [Abstract]

2020 Sep;159:104934. PMID: 32464330
Pharmacol Res

Cordycepin Inhibits Drug-resistance Non-small Cell Lung Cancer Progression by Activating AMPK Signaling Pathway. [Abstract]

2019 Jun:144:79-89. PMID: 30974169
Cancer Lett

Identification and characterization of Bufalin as a novel EGFR degrader. [Abstract]

2025 Apr 10:217715. PMID: 40220852
Cell Death Dis

TRIB2 modulates proteasome function to reduce ubiquitin stability and protect liver cancer cells against oxidative stress. [Abstract]

2021 Jan 7;12(1):42. PMID: 33414446
Osteoarthritis Cartilage

Synovial fluid from end-stage osteoarthritis induces proliferation and fibrosis of articular chondrocytes via MAPK and RhoGTPase signaling. [Abstract]

2022 Jun;30(6):862-874. PMID: 35176481
J Pharm Anal

Development of a competitive enzyme-linked immunosorbent assay for therapeutic drug monitoring of afatinib. [Abstract]

2019 Feb;9(1):49-54. PMID: 30740257
Acta Pharmacol Sin

143D, a novel selective KRASG12C inhibitor exhibits potent antitumor activity in preclinical models. [Abstract]

2023 Jul;44(7):1475-1486. PMID: 36725884
EMBO Mol Med

Upfront admixing antibodies and EGFR inhibitors preempts sequential treatments in lung cancer models. [Abstract]

2021 Apr 9;13(4):e13144. PMID: 33660397
NPJ Parkinsons Dis

EGFR phosphorylates DNAJB1 to suppress α-synuclein aggregation in Parkinson's disease. [Abstract]

2025 Jun 7;11(1):157. PMID: 40483356
ACS Appl Mater Interfaces

Intelligent Biomimetic Nanoplatform for Systemic Treatment of Metastatic Triple-Negative Breast Cancer via Enhanced EGFR-Targeted Therapy and Immunotherapy. [Abstract]

2022 May 25;14(20):23152-23163. PMID: 35549005
NPJ Precis Oncol

High-throughput screening identifies NT-1 that synergizes with MRTX1133 against acquired resistant KRASG12D colorectal cancer. [Abstract]

2026 Apr 8;10(1):211. PMID: 41951768
J Transl Med

Combined treatment with inhibitors of ErbB Receptors and Hh signaling pathways is more effective than single treatment in reducing the growth of malignant mesothelioma both in vitro and in vivo. [Abstract]

2022 Jun 25;20(1):286. PMID: 35752861
Oncogene

Suppression of heparan sulfation re-sensitizes YAP1-driven melanoma to MAPK pathway inhibitors. [Abstract]

2022 Aug;41(32):3953-3968. PMID: 35798875
Oncogene

Epigenetic silencing of miR-483-3p promotes acquired gefitinib resistance and EMT in EGFR-mutant NSCLC by targeting integrin β3. [Abstract]

2018 Aug;37(31):4300-4312. PMID: 29717264
Clin Transl Med

Multi-omic profiling defines three distinct molecular subtypes of urothelial carcinoma with implications for precision therapy. [Abstract]

2026 Mar;16(3):e70638. PMID: 41804750
Sci Signal

TSHZ2 is an EGF-regulated tumor suppressor that binds to the cytokinesis regulator PRC1 and inhibits metastasis. [Abstract]

2021 Jun 22;14(688):eabe6156. PMID: 34158398
Acta Neuropathol Commun

Identifying and exploiting combinatorial synthetic lethality by characterizing adaptive kinome rewiring of EGFRvIII-driven glioblastoma. [Abstract]

2025 Jun 28;13(1):143. PMID: 40581663
J Mater Chem B

Overcoming ABCG2-mediated multidrug resistance by a mineralized hyaluronan-drug nanocomplex. [Abstract]

2016 Nov 7;4(41):6652-6661. PMID: 32263520
Mol Cancer Ther

Dual Inhibitors of KRASG12D and HSP90 are Effective Against KRASG12D Inhibitor Resistance. [Abstract]

2025 Oct 23. PMID: 41129140
Pharmaceutics

Drug Repurposing for the Identification of Compounds with Anti-SARS-CoV-2 Capability via Multiple Targets. [Abstract]

2022 Jan 12;14(1):176. PMID: 35057070
Mol Cancer Ther

Afatinib Is a New Therapeutic Approach in Chordoma with a Unique Ability to Target EGFR and Brachyury. [Abstract]

2018 Mar;17(3):603-613. PMID: 29237806

Afatinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]

Immunoblot analysis of U-CH1, MUG-Chor1 and Chor-IN-1 cells treated with Afatinib for 2 h or 48 h. Protein cell extracts were resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s for each cell line are reported.

Afatinib purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2018 Mar;17(3):603-613. [Abstract]

Immunoblot analysis of U-CH1 cells treated with the indicated doses of inhibitors (Afatinib, Erlotinib and Lapatinib) for 2 h (upper panel) or 48 h (lower panel). Protein cell extracts were resolved on SDS-PAGE gel and membranes probed with the indicated antibodies. IC₅₀s of the different inhibitors are reported.
Cancer Drug Resist

Novel FAK inhibitors suppress tumor growth and reverse EGFR-TKI resistance in non-small cell lung cancer. [Abstract]

2025 Nov 5:8:57. PMID: 41281943
Biol Direct

In vitro synergistic effect of AXL, FAK and ErbB receptors inhibitors for head and neck cancer. [Abstract]

2025 Jul 2;20(1):77. PMID: 40605022
Cancer Nanotechnol

12, 13 (2021).
Int Immunopharmacol

Afatinib inhibits esophageal squamous cell carcinoma by regulating ferroptosis and NRF2 protein homeostasis. [Abstract]

2026 Mar 1:172:116131. PMID: 41520560
Eur J Pharmacol

Discovery of 4-((3,4-dichlorophenyl)amino)-2-methylquinolin-6-ol derivatives as EGFR and HDAC dual inhibitors. [Abstract]

2023 Dec 5:960:176114. PMID: 37863412
Mol Cancer Res

TAS6417/CLN-081 Is a Pan-Mutation-Selective EGFR Tyrosine Kinase Inhibitor with a Broad Spectrum of Preclinical Activity against Clinically Relevant EGFR Mutations. [Abstract]

2019 Nov;17(11):2233-2243. PMID: 31467113
Toxicology

EGFR-TKIs induce acneiform rash and xerosis via Caspase-3/GSDME-mediated pyroptosis of keratinocytes and sebocytes. [Abstract]

2024 Nov 26:154018. PMID: 39608440
Cancers (Basel)

Evaluation of Combined Chemotherapy and Genomic-Driven Targeted Therapy in Patient-Derived Xenografts Identifies New Therapeutic Approaches in Squamous Non-Small-Cell Lung Cancer Patients. [Abstract]

2024 Aug 7;16(16):2785. PMID: 39199558
Cancer Sci

Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. [Abstract]

2018 Apr;109(4):1166-1176. PMID: 29465762

Afatinib purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2018 Apr;109(4):1166-1176. [Abstract]

Influence of Afatinib or Neratinib on human epidermal growth factor receptor 2 (HER2) and the downsignal pathway in gastric cancer cell lines.
Adv Ther

2024 Jul 18.
Sci Rep

A novel human acute myeloid leukemia cell line SDEY-AML1 with KMT2A: MLLT3, IKZF1: EVX1 fusions exhibits high tumorigenicity in NSG mice. [Abstract]

2026 Feb 8;16(1):7792. PMID: 41656387
PLoS Comput Biol

[The epidemiology of arterial hypertension]. [Abstract]

2020 Feb 26;16(2):e1007701. PMID: 2101536
Viruses

Screening and Identification of Lujo Virus Inhibitors Using a Recombinant Reporter Virus Platform. [Abstract]

2021 Jun 28;13(7):1255. PMID: 34203149
Exp Cell Res

Network-based analysis with primary cells reveals drug response landscape of acute myeloid leukemia. [Abstract]

2020 Aug 1;393(1):112054. PMID: 32376287
Cell Biol Int

Sensitization of HT29 colorectal cancer cells to vemurafenib in three-dimensional collagen cultures. [Abstract]

2020 Feb;44(2):621-629. PMID: 31736196
J Pharm Biomed Anal

Comparative studies on the human serum albumin binding of the clinically approved EGFR inhibitors gefitinib, erlotinib, afatinib, osimertinib and the investigational inhibitor KP2187. [Abstract]

2018 May 30:154:321-331. PMID: 29567575
Genes (Basel)

The Impact of Bevacizumab and miR200c on EMT and EGFR-TKI Resistance in EGFR-Mutant Lung Cancer Organoids. [Abstract]

2024 Dec 19;15(12):1624. PMID: 39766891
PLoS One

A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]

2024 Nov 1;19(11):e0308647. PMID: 39485774
PLoS One

DSE promotes aggressive glioma cell phenotypes by enhancing HB-EGF/ErbB signaling. [Abstract]

2018 Jun 4;13(6):e0198364. PMID: 29864158
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
Int J Radiat Biol

Celecoxib and Afatinib synergistic enhance radiotherapy sensitivity on human non-small cell lung cancer A549 cells. [Abstract]

2021;97(2):170-178. PMID: 33164600
Acta Histochem

Immunohistochemical localization of afatinib in male rat intestines and skin after its oral administration. [Abstract]

2019 Nov;121(8):151439. PMID: 31500866
GEN Biotechnol

2025 Apr 17.
J Oral Biosci

Antihypertensive agent losartan promotes tongue squamous cell carcinoma cell proliferation via EGFR/ERK1/2/cyclin D1 signaling axis. [Abstract]

2024 Sep 6:S1349-0079(24)00198-1. PMID: 39245205
Biochem Biophys Res Commun

2026 Feb 12:800:153165. PMID: 41548485

Afatinib purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2026 Feb 12:800:153165.

ActE_21 binding to A549, SK-BR-3 and A431 after incubation with Afatinib (Afatinib dimaleate; 50 nM) for 120 min at 37 °C. Afatinib increases EGF-EGFR complex surface levels in A549 and SK-BR-3 cell.
Oncol Lett

EGFR and ERK activation resists flavonoid quercetin-induced anticancer activities in human cervical cancer cells in vitro. [Abstract]

2021 Nov;22(5):754. PMID: 34539858
Cryobiology

Cryoprotectant toxicity in Caenorhabditis elegans. [Abstract]

2019 Feb:86:71-76. PMID: 30527584
Cell Physiol Biochem

Stimulation of Eryptosis by Afatinib. [Abstract]

2018;47(3):1259-1273. PMID: 29913444
Bioanalysis

Development and validation of an ELISA with high sensitivity for therapeutic monitoring of afatinib. [Abstract]

2018 Sep 1;10(18):1511-1523. PMID: 30117333
Biomed Chromatogr

Simultaneous and rapid determination of gefitinib, erlotinib and afatinib plasma levels using liquid chromatography/tandem mass spectrometry in patients with non-small-cell lung cancer. [Abstract]

2016 Jul;30(7):1150-4. PMID: 26525154
Biol Methods Protoc

Optimizing drug sensitivity assays in patient-derived tumor organoids: a comparison of IC50 estimation methods and experimental parameters. [Abstract]

2025 Feb 13;10(1):bpaf012. PMID: 40060949
Xenobiotica

Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1. [Abstract]

2018 Oct;48(10):1059-1071. PMID: 29034773
bioRxiv

2026 Jun 19.
bioRxiv

2026 Mar 12.
bioRxiv

2026 Jan 9.
bioRxiv

2026 Jan 12.
Technical University of Dresden

2025.
bioRxiv

2025 Dec 5.
bioRxiv

2025 Nov 24.
SSRN

2025 Jul 4.
bioRxiv

Modeling acquired TKI resistance and effective combination therapeutic strategies in murine RET+ lung adenocarcinoma. [Abstract]

2025 Jun 7:2025.06.04.657911. PMID: 40502048
World J Exp Med

Establishment and characterization of a new human gallbladder cancer cell line, OCUG-2. [Abstract]

2025 Jun 20;15(2):100443. PMID: 40546672
State University of New York at Buffalo

2025.
bioRxiv

BRAFV600E-Driven Lung Tumorigenesis Requires Ligand-Mediated Activation of ERBB Receptor Signaling. [Abstract]

2025 May 9:2025.05.04.652129. PMID: 40654950

Afatinib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

Afatinib dimaleate (15 mg/kg; oral gavage; once daily for 8 weeks) reduced tumor burden and tumor diameter in Braf^CAT mice.

Afatinib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

Afatinib dimaleate (Afatinib; 15 mg/kg; oral gavage; once daily for 8 weeks). Immunohistochemistry analyses of phosphorylated ERK (pT202, Y204) in Braf^CAT formalin fixed paraffin embedded (FFPE) mouse lung tissue.

Afatinib purchased from MedChemExpress. Usage Cited in: bioRxiv. 2025 May 9:2025.05.04.652129. [Abstract]

Afatinib dimaleate (A; 50 nM; 2 or 24 h), alone or in combination with dabrafenib and trametinib (D+T+A), enhances pathway blockade in HCC364 human BRAF^V600E+ lung cancer cells.
Patent

US20240344020A1
Patent

US20240344020A1.
bioRxiv

2024 October 04.
Research Square Preprint

2024 Nov 26.
bioRxiv

2024 Feb 12.
bioRxiv

Structural dynamics of the active HER4 and HER2/HER4 complexes is finely tuned by different growth factors and glycosylation. [Abstract]

2024 Jan 4:2023.10.06.561161. PMID: 38260342
University of Cádiz

2023 Oct.
bioRxiv

2023 Sep 13.
Research Square Print

2023 Jan 6.
bioRxiv

October 28, 2021.
Research Square Preprint

2021 Jul.
Chem Rep

2019, 1(1): 3-12.
Patent

US20190010159A1.
Oncotarget

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells. [Abstract]

2015 Oct 13;6(31):31313-22. PMID: 26375053
Oncotarget

Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. [Abstract]

2014 Dec 15;5(23):11971-85. PMID: 25436978

Afatinib purchased from MedChemExpress. Usage Cited in: Oncotarget. 2014 Dec 15;5(23):11971-85. [Abstract]

H460/MX20 cells are treated with varying concentrations (0–2.0 μM) of Afatinib for 48 h, or with 1.0 μM Afatinib for 24 h, 48 h and 72 h, respectively. ABCG2 protein levels are analyzed by Western blot. GAPDH is used as a loading control.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (205.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.0579 mL

10.2893 mL

20.5787 mL

5 mM

0.4116 mL

2.0579 mL

4.1157 mL

10 mM

0.2058 mL

1.0289 mL

2.0579 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% Methylcellulose/saline water

Solubility: 5 mg/mL (10.29 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (289 KB)
SDS (557 KB)
- English - EN (557 KB)
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- Deutsch - DE (557 KB)
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- Italian - IT (557 KB)
- Portuguese - PT (557 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Li D, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11. [Content Brief]

[2]. Wong CH, et al. Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC). Am J Cancer Res. 2015 Nov 15;5(12):3588-99. [Content Brief]

[3]. Wang XK, et al. Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. Oncotarget. 2014 Dec 15;5(23):11971-85. [Content Brief]

[4]. Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0579 mL	10.2893 mL	20.5787 mL	51.4467 mL
	5 mM	0.4116 mL	2.0579 mL	4.1157 mL	10.2893 mL
	10 mM	0.2058 mL	1.0289 mL	2.0579 mL	5.1447 mL
	15 mM	0.1372 mL	0.6860 mL	1.3719 mL	3.4298 mL
	20 mM	0.1029 mL	0.5145 mL	1.0289 mL	2.5723 mL
	25 mM	0.0823 mL	0.4116 mL	0.8231 mL	2.0579 mL
	30 mM	0.0686 mL	0.3430 mL	0.6860 mL	1.7149 mL
	40 mM	0.0514 mL	0.2572 mL	0.5145 mL	1.2862 mL
	50 mM	0.0412 mL	0.2058 mL	0.4116 mL	1.0289 mL
	60 mM	0.0343 mL	0.1715 mL	0.3430 mL	0.8574 mL
	80 mM	0.0257 mL	0.1286 mL	0.2572 mL	0.6431 mL
	100 mM	0.0206 mL	0.1029 mL	0.2058 mL	0.5145 mL

Afatinib

107 Cited Publications

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Afatinib

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