Cat. No.: HY-10261B

(E/Z)-Afatinib

(Synonyms: (E/Z)-BIBW 2992)

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(E/Z)-Afatinib ((E/Z)-BIBW 2992) is the mixture of (E)-Afatinib and (Z)-Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells.

For research use only. We do not sell to patients.

Purity: 99.98%
CAS No.: 439081-18-2
Formula: C₂₄H₂₅ClFN₅O₃
Molecular Weight:485.94

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

(E/Z)-Afatinib Chemical Structure

CAS No.: 439081-18-2

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Biological Activity
- Description
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- In Vitro
Chemical Information
Publications (1)
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Biological Activity

Description

All EGFR Isoforms :

All Akt Isoforms :

All p38 MAPK Isoforms :

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]
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	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]
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]
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/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay	[PMID: 23930994]
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-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	0.1 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]
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

Potent, irreversible Her2/ErbB 2 and EGFR kinase inhibitor

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

Chemical Information

CAS No. 439081-18-2
Appearance Solid
Molecular Weight 485.94
Formula C₂₄H₂₅ClFN₅O₃
Color White to off-white
SMILES

O=C(/C=C/CN(C)C)NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1O[C@@H]4COCC4
Synonyms

(E/Z)-BIBW 2992
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Cell Rep Methods

Tumor immune microenvironment reconstitution in patient-derived organoids enables therapy modeling for NSCLC. [Abstract]

2026 Jun 15;6(6):101339. PMID: 42134319

Solvent & Solubility

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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Handling Instructions (2659 KB)

References

[1]. 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]

[2]. 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]

[3]. 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]

[4]. 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]

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

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

Keywords

(E/Z)-Afatinib

1 Cited Publications

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(E/Z)-Afatinib

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Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

(E/Z)-Afatinib Related Classifications

HY-10261B Related Classifications