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

目录号: HY-10261B 纯度: 99.98%: FAQs
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(E/Z)-Afatinib ((E/Z)-BIBW 2992) 是 (E)-Afatinib 和 (Z)-Afatinib 的混合物。Afatinib (HY-10261) 是一种不可逆的 EGFR 抑制剂，通过不可逆地与其 ATP 结合位点结合来阻断 EGFR、HER2、HER4 和 EGFRvIII 的激活。 Afatinib 与 Temozolomide (HY-17364) 联合给药，有效靶向胶质母细胞瘤细胞中的 EGFRvIII-cMet 信号传导。

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(E/Z)-Afatinib Chemical Structure

CAS No. : 439081-18-2

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥194	In-stock
100 mg	￥176	In-stock
250 mg	￥352	In-stock
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1 g		询价

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Other Forms of (E/Z)-Afatinib:

Afatinib oxalate 询价
(E/Z)-Afatinib (Standard) 询价

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生物活性
纯度 & 产品资料
参考文献

生物活性

(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^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
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	0.023 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	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	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]
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	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	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	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]
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	0.71 μM Compound: Afatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
A549	IC₅₀	1.33 μM Compound: Afatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
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	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	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	6.34 μM Compound: Afatinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
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	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	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	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]
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	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	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]
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]
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]
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]
HepG2	IC₅₀	1.16 μM Compound: Afatinib	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
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	1.4 μM Compound: Afatinib	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
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]
MCF7	IC₅₀	0.93 μM Compound: Afatinib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
MCF7	IC₅₀	1.09 μM Compound: Afatinib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
MCF7	IC₅₀	2.63 μM Compound: Afatinib	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
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	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	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	0.148 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	0.37 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	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	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	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	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	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	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	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	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	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	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	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	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	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-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]
PC-3	IC₅₀	1.13 μM Compound: Afatinib	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
PC-3	IC₅₀	2.52 μM Compound: Afatinib	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 32739648]
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-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-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	0.00057 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	0.1 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	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]
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]

体外研究
(In Vitro)

有效、不可逆的 Her2/ErbB 2 和 EGFR 激酶抑制剂

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

分子量

485.94

Formula

C₂₄H₂₅ClFN₅O₃

CAS 号

439081-18-2

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (205.79 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.14 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.14 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

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

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.98%

选择批次：

Data Sheet (621 KB) SDS (393 KB)

COA (287 KB) HNMR (127 KB) LCMS (228 KB)

产品使用指南 (1538 KB)

参考文献

[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]

(E/Z)-Afatinib 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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

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

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