Afatinib (BIBW2992) Dimaleate

Name: Afatinib (BIBW2992) Dimaleate
Brand: Selleck Chemicals
SKU: S7810
Rating: 5 (99 reviews)

For research use only.

Catalog No.S7810

99 publications

Afatinib (BIBW2992) Dimaleate Chemical Structure

CAS No. 850140-73-7

Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Afatinib (BIBW2992) Dimaleate induces autophagy.

Selleck's Afatinib (BIBW2992) Dimaleate has been cited by 99 publications

Cancer Cell, 2020, 37(2):183-199

PubMed: 31978326 ( click the link to review the publication )

Cancer Discov, 2017, 7(6):575-585

PubMed: 28274957 ( click the link to review the publication )

Cancer Discov, 2013, 3(2):168-81

PubMed: 23229345 ( click the link to review the publication )

Theranostics, 2021, 11(6):2594-2611

PubMed: 33456562 ( click the link to review the publication )

Mol Cancer, 2021, 20(1):17

PubMed: 33461557 ( click the link to review the publication )

Drug Metab Dispos, 2021, 49(1):53-61

PubMed: 33148688 ( click the link to review the publication )

Clin Cancer Res, 2020, clincanres.3555.2020

PubMed: 33355298 ( click the link to review the publication )

Genome Med, 2020, 18;12(1):17

PubMed: 32070411 ( click the link to review the publication )

Oncogene, 2020, 10.1038/s41388-020-01564-w

PubMed: 33288882 ( click the link to review the publication )

Oncogene, 2020, 39(20):3997-4013

PubMed: 32242147 ( click the link to review the publication )

J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X

PubMed: 32376279 ( click the link to review the publication )

Cancers (Basel), 2020, 13;12(2) pii: E436

PubMed: 32069833 ( click the link to review the publication )

Cancers (Basel), 2020, 12(12)E3869

PubMed: 33371412 ( click the link to review the publication )

Cell Death Dis, 2020, 11(10):882

PubMed: 33082316 ( click the link to review the publication )

Signal Transduct Target Ther, 2020, 5(1):214

PubMed: 33033232 ( click the link to review the publication )

Oral Oncol, 2020, 112:105074

PubMed: 33142224 ( click the link to review the publication )

J Virol, 2020, JVI.02001-20

PubMed: 33361428 ( click the link to review the publication )

Antimicrob Agents Chemother, 2020, 1;AAC.00341-20

PubMed: 32482675 ( click the link to review the publication )

Sci Rep, 2020, 10(1):17768

PubMed: 33082482 ( click the link to review the publication )

J Biol Chem, 2020, jbc.RA120.015891

PubMed: 33087447 ( click the link to review the publication )

Am J Transl Res, 2020, 15;12(3):847-856 eCollection 2020

PubMed: 32269717 ( click the link to review the publication )

Cancer Res Treat, 2020, 10.4143/crt.2020.585

PubMed: 33070556 ( click the link to review the publication )

Toxicol In Vitro, 2020, 104928

PubMed: 32622998 ( click the link to review the publication )

Oncol Rep, 2020, 44(6):2581-2594

PubMed: 33125153 ( click the link to review the publication )
PLoS One, 2020, 15(1):e0227261

PubMed: 31914141 ( click the link to review the publication )

Hum Cell, 2020, 10.1007/s13577-020-00420-z

PubMed: 32870449 ( click the link to review the publication )

Anticancer Res, 2020, 40(4):1867-1874

PubMed: 32234874 ( click the link to review the publication )

Korean J Parasitol, 2020, 58(3):249-255

PubMed: 32615738 ( click the link to review the publication )

Neurooncol Adv, 2020, Dec;2(1):vdaa020

PubMed: 32226941 ( click the link to review the publication )

Sci Rep, 2020, 10(1):12982

PubMed: 32737414 ( click the link to review the publication )

BMC Pharmacol Toxicol, 2020, 21(1):61

PubMed: 32795383 ( click the link to review the publication )

NPJ Breast Cancer, 2020, 6:30

PubMed: 32715085 ( click the link to review the publication )

Physiol Rep, 2020, 8(13):e14490

PubMed: 32652816 ( click the link to review the publication )

J Cell Physiol, 2020, 10.1002/jcp.30172

PubMed: 33230821 ( click the link to review the publication )

Rapid Commun Mass Spectrom, 2020, 10.1002/rcm.8955

PubMed: 32990383 ( click the link to review the publication )

Cancer Cell Int, 2020, 20:376

PubMed: 32774169 ( click the link to review the publication )

Circulation, 2019, 139(22):2570-2584

PubMed: 30922063 ( click the link to review the publication )

Oncoimmunology, 2019,

PubMed: 30713780 ( click the link to review the publication )

Sci Rep, 2019,

PubMed: 31882684 ( click the link to review the publication )

EMBO Mol Med, 2018, 10(9):e8746

PubMed: 30021798 ( click the link to review the publication )

Clin Cancer Res, 2018, 24(5):1227-1239

PubMed: 29229632 ( click the link to review the publication )

Clin Cancer Res, 2018, 15;24(6):1436-1447

PubMed: 29127119 ( click the link to review the publication )

Cell Death Dis, 2018,

PubMed: 29880898 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(8):1648-1658

PubMed: 29748209 ( click the link to review the publication )

J Thorac Oncol, 2017, 12(5):884-889

PubMed: 28088511 ( click the link to review the publication )

Theranostics, 2017, 7(4):974-986

PubMed: 28382169 ( click the link to review the publication )

Oncogene, 2017, 36(47):6581-6591

PubMed: 28783173 ( click the link to review the publication )

Arch Toxicol, 2017, 91(8):2921-2938

PubMed: 28032146 ( click the link to review the publication )
Mol Cancer Ther, 2017,

PubMed: 27913578 ( click the link to review the publication )

BMC Cancer, 2017,

PubMed: 28806950 ( click the link to review the publication )

Oncotarget, 2017, 8(3):4277-4288

PubMed: 28032592 ( click the link to review the publication )

Oncotarget, 2017, 8(14):22414-22432

PubMed: 26461472 ( click the link to review the publication )

Oncotarget, 2017,

PubMed: 29050315 ( click the link to review the publication )

Oncotarget, 2017,

PubMed: 28423495 ( click the link to review the publication )

Mol Cancer Ther, 2016,

PubMed: 27207775 ( click the link to review the publication )

Mol Cancer Ther, 2016,

PubMed: 27678331 ( click the link to review the publication )

Cancer Sci, 2016, 107(8):1134-40

PubMed: 27240419 ( click the link to review the publication )

Cancer Immunol Res, 2016,

PubMed: 27799141 ( click the link to review the publication )

Cancer Immunol Res, 2016,

PubMed: 27680026 ( click the link to review the publication )

Oncotarget, 2016,

PubMed: 26623721 ( click the link to review the publication )

Gut, 2015, 10.1136/gutjnl-2014-309026

PubMed: ( click the link to review the publication )

Nat Commun, 2015, 6:8481

PubMed: 26412466 ( click the link to review the publication )

Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-14-2789

PubMed: 25948633 ( click the link to review the publication )

Clin Cancer Res, 2015, 10.1158/1078-0432.CCR-15-0560

PubMed: 25964297 ( click the link to review the publication )

Int J Cancer, 2015, 136(11):2717-29

PubMed: ( click the link to review the publication )

J Med Chem, 2015, 58(16):6589-606

PubMed: 26258521 ( click the link to review the publication )

Cancer Discov, 2015,

PubMed: 26243863 ( click the link to review the publication )

Mol Cancer Ther, 2015, 10.1158/1535-7163.MCT-13-0951

PubMed: 25589492 ( click the link to review the publication )

Antimicrob Agents Chemother, 2015, 59(2):1088-99

PubMed: 25487801 ( click the link to review the publication )

Antimicrob Agents Chemother, 2015, 59(2):1088-99

PubMed: ( click the link to review the publication )

Drug Metab Dispos, 2015, 43(3):375-84

PubMed: ( click the link to review the publication )

Drug Metab Dispos, 2015, 43(3):375-84

PubMed: 25504185 ( click the link to review the publication )
Cell Tissue Res, 2015, 359(3):799-816

PubMed: ( click the link to review the publication )

Oncol Rep, 2015,

PubMed: 26503698 ( click the link to review the publication )

Arch Immunol Ther Exp, 2015, 63(3):207-14

PubMed: 25678473 ( click the link to review the publication )

PLoS ONE, 2015,

PubMed: 25969993 ( click the link to review the publication )

Anticancer Res, 2015, 35(4):2005-8

PubMed: 25862853 ( click the link to review the publication )

Oncotarget, 2015,

PubMed: 25686822 ( click the link to review the publication )

Oncotarget, 2015,

PubMed: 25965827 ( click the link to review the publication )

Oncotarget, 2015,

PubMed: 25537503 ( click the link to review the publication )

Nat Commun, 2014, 5:5232

PubMed: 25366117 ( click the link to review the publication )

J Natl Cancer Inst, 2014, 106(9)

PubMed: 25214559 ( click the link to review the publication )

Clin Cancer Res, 2014, 20(21):5423-34

PubMed: 25189483 ( click the link to review the publication )

Drug Metab Dispos, 2014, 42(11):1851-7

PubMed: 25165131 ( click the link to review the publication )

Histochem Cell Biol, 2014, 142(4):361-71

PubMed: 24824474 ( click the link to review the publication )

Target Oncol, 2014, 10.1007/s11523-014-0344-7

PubMed: 25341405 ( click the link to review the publication )

Oncotarget, 2014, 5(24):12877-90

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Assay Drug Dev Technol, 2014, 12(9-10):514-26

PubMed: 25506801 ( click the link to review the publication )

Oncotarget, 2014, 5(15):5908-19

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Genes Cancer, 2014, 5(7-8):261-72

PubMed: 25221644 ( click the link to review the publication )

Eur J Cancer, 2013, 49(6):1458-66

PubMed: 23153706 ( click the link to review the publication )

Oncogene, 2013, 32(37):4427-35

PubMed: 23045273 ( click the link to review the publication )

Cancer Sci, 2013, 104(12):1618-25

PubMed: 24112719 ( click the link to review the publication )

Evid Based Complement Alternat Med, 2013, 2013:243859

PubMed: 23533466 ( click the link to review the publication )

J Thorac Oncol, 2012, 7(2):272-80

PubMed: 22089117 ( click the link to review the publication )

Clin Cancer Res, 2012, 18(6):1663-71

PubMed: 22317763 ( click the link to review the publication )
PLoS One, 2012, 7(7):e41017

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Oncol Res, 2011, 19(10-11):471-8

PubMed: 22715590 ( click the link to review the publication )

Int J Proteomics, 2011, 2011:215496

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Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description

Targets

EGFR (L858R) ^[1] (Cell-free assay)	EGFR (wt) ^[1] (Cell-free assay)	EGFR (L858R/T790M) ^[1] (Cell-free assay)	HER2 ^[1] (Cell-free assay)
0.4 nM	0.5 nM	10 nM	14 nM

In vitro

BIBW2992 is more effective than erlotinib, geﬁtinib, or lapatinib in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR. BIBW2992 is similarly effective against NSCLC lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), but shows no activity toward A549 cells, which express wild-type EGFR and HER2.^[1] Afatinib enhances cytotoxicity of topotecan and mitoxantrone to SP cells, and increases the apoptosis induced by topotecan and mitoxantrone in SP cells.^[2]

Cell Data

Cell Lines	Assay Type	Incubation Time	Activity Description	PMID
HCC827 cell	MUfQdo9tcW[ncnH0bY9vKGG\|c3H5		M37oZmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPDPFI4KGOnbHzzJIFnfGW{IEm2JIhzeyCkeTDNWHMh[XO\|YYmsJGlEPTB;ODDuUS=>	MUKyNFU2ODJzMh?=
NCI-H1563	MkDjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NGn3cXRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVU3OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LjDJR\|UxRTlwN{[wN\|Eh\|ryP	M1TvT3NCVkeHUh?=
NCI-H1573	NIHLNWlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NF;od2xKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVU4OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LjDJR\|UxRTBwN{O2N{DPxE1?	MV\TRW5ITVJ?
NCI-H1581	MoPzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MXXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUW4NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVI6NjNzNEWg{txO	NGqzWmpUSU6JRWK=
NCI-H1648	NIrDcHNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NYXISFJFUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3PDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeT6gTWM2OD1yLkS0NVgzKM7:TR?=	M{TjVHNCVkeHUh?=
NCI-H1793	Moe5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M3\MOGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixO\|k{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XlwIFnDOVA:OTRwMkC4O{DPxE1?	M2W1e3NCVkeHUh?=
NCI-H1838	NF\OWIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MVnJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUizPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVAvPjB{OUmg{txO	NYXLZmtZW0GQR1XS
NCI-H1770	NWXUSllNT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NWG2PJdmUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE4PzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeT6gTWM2OD1yLkGwNlgh\|ryP	MofDV2FPT0WU
NCI-H1651	MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MnXRTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0zPS53OUeg{txO	MoPBV2FPT0WU
NCI-H1975	MnTUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MnP6TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG5O\|Uh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0xNjZzN{K4JO69VQ>?	NXuxeZAyW0GQR1XS
NCI-H1666	M1PLfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MlmyTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG2OlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0yNjhyOUS4JO69VQ>?	M{m5OXNCVkeHUh?=
NCI-H2009	NILYfm5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MoDiTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0{NjZzMkG2JO69VQ>?	MkTZV2FPT0WU
NCI-H2126	NGf0XJdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M2PXVWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNVI3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XlwIFnDOVA:OC53MUmyOkDPxE1?	NVHJNnlIW0GQR1XS
NCI-H1693	MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		NYHNbI41UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE3QTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeT6gTWM2OD1\|Lki0NVgyKM7:TR?=	NHvBd5RUSU6JRWK=
NCI-H2087	M4T2R2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MXjJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkC4O{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVQ6Njl4OEKg{txO	Mn65V2FPT0WU
NCI-H2029	M1TZT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MnSwTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF01Oy53NUixJO69VQ>?	M3v2cHNCVkeHUh?=
NCI-H2170	MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		Mnr1TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKxO\|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0xNjB\|N{K4JO69VQ>?	M37O[HNCVkeHUh?=
NCI-H226	MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M1XGc2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNlYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF01QS55N{i1JO69VQ>?	MX3TRW5ITVJ?
NCI-H2030	NHjpcGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MmnKTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwN\|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0yPC54NES4JO69VQ>?	M2TxPXNCVkeHUh?=
NCI-H2052	NXrIOZV2T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		MWTJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkC1NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVIyNjh7NkOg{txO	MV7TRW5ITVJ?
NCI-H292	MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MXjJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkmyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9NE4xPjB7IN88US=>	MYXTRW5ITVJ?
NCI-H441	NHLDZ5dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M37CbWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi0OFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0{NjV7OESxJO69VQ>?	MUXTRW5ITVJ?
NCI-H2291	MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MXHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMkK5NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVUvQTh7NEOg{txO	M4jwRnNCVkeHUh?=
NCI-H358	MmnTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MUHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KM{W4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9NE42OzJzIN88US=>	NU\BeYhsW0GQR1XS
NCI-H460	MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MX7Jcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNE[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9OFYvPTJ\|IN88US=>	NILVSVFUSU6JRWK=
NCI-H661	NGfHb2dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M{X2WGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi2OlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0yPi57Nkm0JO69VQ>?	NXvKZ5JpW0GQR1XS
NCI-H23	NGrFNZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NF;4c5RKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0{Py52MUm2JO69VQ>?	M2TsVHNCVkeHUh?=
NCI-H630	NF7yb2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MVPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNkOwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9NU41PTV6MjFOwG0>	NV60[lliW0GQR1XS
NCI-H2342	M2ezSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M1XQb2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyN\|QzKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XlwIFnDOVA:OTdwNUW3JO69VQ>?	M2eyOnNCVkeHUh?=
NCI-H69	NHruWm9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=		Mo\sTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSE[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9NE4zOTR3MTFOwG0>	NEDxeGVUSU6JRWK=
NCI-H650	MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		M4LK[2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVi2OVAh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0yOS5{NEG4JO69VQ>?	MXjTRW5ITVJ?
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NCI-H1755	NFrtNZhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NVT2VplkUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE4PTViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeT6gTWM2OD12MT64O\|I2KM7:TR?=	MWLTRW5ITVJ?
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OVCAR-3	MnjQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M2jmRmlvcGmkaYTpc44hd2ZiaIXtZY4hV1[FQWKtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVIvPjdzNkeg{txO	MYfTRW5ITVJ?
OVCAR-4	NE[xe4NIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MUfJcohq[mm2aX;uJI9nKGi3bXHuJG9XS0GULUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME2xNE45QDN3IN88US=>	NIDVSWpUSU6JRWK=
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BALL-1	M4C0S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NF25eFFKdmirYnn0bY9vKG:oIHj1cYFvKEKDTFytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVkvOjF7MEeg{txO	NVnafGRVW0GQR1XS
BB65-RCC	M3fTN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M2jtZWlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ4NT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0xNjN2NUmzJO69VQ>?	NVvHUWdwW0GQR1XS
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BHT-101	NHHEUIVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MWPJcohq[mm2aX;uJI9nKGi3bXHuJGJJXC1zMEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME2xOE4zPDFizszN	NUXWTIRHW0GQR1XS
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SW684	Mo\rS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NXu5dGUxUW6qaXLpeIlwdiCxZjDoeY1idiCVV{[4OEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVE6NjF\|Mk[g{txO	MkfHV2FPT0WU
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SW780	Ml\GS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		M1jKbGlvcGmkaYTpc44hd2ZiaIXtZY4hW1d5OECgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME2yOU4{OjZ2IN88US=>	M3H5PHNCVkeHUh?=
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SK-LMS-1	Mmi0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		MWLJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyPUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9OVEvQThzNTFOwG0>	NITHXYVUSU6JRWK=
SK-MEL-30	MkmzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?		NXrSeotnUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeT6gTWM2OD1zM{OuOFgyKM7:TR?=	NF65WmVUSU6JRWK=
SNB75	NVnUfVl5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NIrrPJZKdmirYnn0bY9vKG:oIHj1cYFvKFOQQke1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9OVAvPDF2IN88US=>	NVu0U3R4W0GQR1XS
SNU-423	M4OyRWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MmDETY5pcWKrdHnvckBw\iCqdX3hckBUVlVvNEKzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9O\|AvPjBzNzFOwG0>	NXXhe5dCW0GQR1XS
SW1088	M3TkTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MkLJTY5pcWKrdHnvckBw\iCqdX3hckBUXzFyOEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME21NE4xOjBzIN88US=>	NGrhSFNUSU6JRWK=
SW1783	NGmxV5FIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M2jnTGlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{izJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9OVIvPDl6MjFOwG0>	Ml3vV2FPT0WU
SBC-5	NGi0WGJIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NVLGZoFTUW6qaXLpeIlwdiCxZjDoeY1idiCVQlOtOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVUyNjFyOEWg{txO	Ml7aV2FPT0WU
A375	NHLLU\|BIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M3q3ZmlvcGmkaYTpc44hd2ZiaIXtZY4hSTN5NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MkBKSzVyPUWzMlY4PjhizszN	MlrxV2FPT0WU
AM-38	NVvaVnZnT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=		NU\JU2pwUW6qaXLpeIlwdiCxZjDoeY1idiCDTT2zPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVUzNjl2OUKg{txO	Mnq2V2FPT0WU
YH-13	M3;vSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		MXPJcohq[mm2aX;uJI9nKGi3bXHuJHlJNTF\|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmuJGlEPTB;NkCuNFQ3QCEQvF2=	MlK1V2FPT0WU
TYK-nu	NGGxUWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NFvzTWFKdmirYnn0bY9vKG:oIHj1cYFvKFS\Sz3ueUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVc3NjZyNkOg{txO	MY\TRW5ITVJ?
COLO-668	M4LRS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NYrv[Is4UW6qaXLpeIlwdiCxZjDoeY1idiCFT1zPMVY3QCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LjDJR\|UxRTZyLkWwO\|ch\|ryP	MU\TRW5ITVJ?
ES6	NGG1TmZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NYjKV5dwUW6qaXLpeIlwdiCxZjDoeY1idiCHU{[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME21O{44PTRzIN88US=>	NXq4S2dyW0GQR1XS
D-247MG	MX;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?		MYTJcohq[mm2aX;uJI9nKGi3bXHuJGQuOjR5TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME21PU42QDh6IN88US=>	MlLnV2FPT0WU
H4	NGDvZXRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		MUDJcohq[mm2aX;uJI9nKGi3bXHuJGg1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XlwIFnDOVA:PjBwNU[xOEDPxE1?	Mom1V2FPT0WU
HMV-II	M1\SV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M2XDc2lvcGmkaYTpc44hd2ZiaIXtZY4hUE2YLVnJJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9NVU4NjF7NDFOwG0>	NHjqR2NUSU6JRWK=
HT-1080	NHvQWXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		M4LHc2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMUC4NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVYzNjJyMzFOwG0>	NVG4PJVLW0GQR1XS
IA-LM	M3vrd2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7		M4DvOGlvcGmkaYTpc44hd2ZiaIXtZY4hUUFvTF2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME21OE4xQTFizszN	M4DRT3NCVkeHUh?=
K-562	M4eyWGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NITxeFNKdmirYnn0bY9vKG:oIHj1cYFvKEtvNU[yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZkvKEmFNUC9OVAvPTZ\|MzFOwG0>	NHLHVpVUSU6JRWK=
MEL-JUSO	NGDhb5NIem:5dHigbY5pcWKrdHnvckBie3OjeR?=		NVHDT2wxUW6qaXLpeIlwdiCxZjDoeY1idiCPRVytTnVUVyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LjDJR\|UxRTV4LkG3N\|ch\|ryP	NGW4eYVUSU6JRWK=
M059J	M2q3PWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NUH1TWcxUW6qaXLpeIlwdiCxZjDoeY1idiCPMEW5TkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVUyNjB{NUKg{txO	MmrBV2FPT0WU
NB6	M4Tjemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7		NYK1WW9lUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfU4hUUN3ME23NU4xPzl5IN88US=>	MYTTRW5ITVJ?
NCI-H1975	MUnQdo9tcW[ncnH0bY9vKGG\|c3H5	MWm3NkBp	NX64eFdlSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDF7N{WgZ4VtdHNiZYjwdoV{e2mwZzDFS2ZTKFR5OUDNJI12fGGwdDDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR\|UxRTBwMUS4JO69VQ>?	NVLISIV4OjRzOEO3OFI>
A431	M2LHcHBzd2yrZnXyZZRqd25iYYPzZZk>	M{XjOFczKGh?	M3mwU2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUSzNUBk\WyuczDh[pRmeiB5MjDodpMh[nliU2LCJIF{e2G7LDDJR\|UxRTBwMEKzJI5O	MlOzNlQyQDN5NEK=
MDA-MB-231	MljUVJJwdGmoZYLheIlwdiCjc4PhfS=>	NGDRbIM4OiCq	MlraRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEWFNUC9NUBvVQ>?	NUHpPJJnOjBzOEC5NFY>
NCI-H1975	MoPGR5l1d3SxeHnjbZR6KGG\|c3H5	Mom1OFghcA>?	NXm5U4lzS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVkOLLVixPVc2KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;MD6zPVIh\|ryP	M33EelIxOTVyNEC0
NIH/3T3	M1Ll[WN6fG:2b4jpZ4l1gSCjc4PhfS=>	NYm5O3FJPDhiaB?=	MkfFR5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgUmlJNzOWMzDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVMvPjB3IN88US=>	NIS3fpEzODF3MESwOC=>
A549	M3;PZmN6fG:2b4jpZ4l1gSCjc4PhfS=>	NUj4NI9NPzJiaB?=	MkHFR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVU1QSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUCuNFUh\|ryP	NWDleGEyOjBzOEC5NFU>
PC3	NHnzfWtEgXSxdH;4bYNqfHliYYPzZZk>	M3;HR\|czKGh?	MoPmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;ND6xJO69VQ>?	MWGyNFE5ODlyNR?=
HeLa	MU\DfZRwfG:6aXPpeJkh[XO\|YYm=	MnnZO\|IhcA>?	MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[WxiKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO\|YYmsJGlEPTB;Nj64NUDPxE1?	MnnqNlAyQDB7MEW=
MCF7	MWLDfZRwfG:6aXPpeJkh[XO\|YYm=	M1[yfFczKGh?	MljmR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWNHPyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyPUWuPFMh\|ryP	M3LRd\|IxOThyOUC1
NSCLC	NVj1S5FkS3m2b4TvfIlkcXS7IHHzd4F6	NH7jcWU4OiCq	MUPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDOV2NNSyClZXzsd{whUUN3ME2wMlUhdk1?	MUeyNFE5ODlyNR?=

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Growth inhibition assay	Cell apoptosis; PubMed: 25537503 Oncotarget Dose-dependent effects of afatinib on apoptosis. Data are mean ± SD. n = 3 for each concentration. , p < 0.05, *, p < 0.01, vs. no afatinib. Cell viability; PubMed: 26515464 Oncotarget A. MTS assay for Ba/F3 cells harboring EGFR exon 19 deletion and L858R. The proportional cell viability is shown. B. MTS assay for Ba/F3 cells harboring EGFR exon 19 deletion+T790M and L858R+T790M. The proportional cell viability is shown. C. MTS assay for Ba/F3 cells harboring wild type EGFR. The proportional cell viability is shown. Erlotinib, afatinib, osimertinib, and rociletinib were used as EGFR-TKIs. Error bars indicate standard deviation.	25537503 26515464
Western blot	CIP2A / p-AKT / AKT / PARP; PubMed: 25537503 Oncotarget Time-dependent effects of afatinib on CIP2A, p-AKT and apoptosis-related proteins in the sensitive H358 and resistant H460 cells. Cells were exposed to 10 μM afatinib for up to 48 hours. Immunoblots were scanned and quantitated to determine the ratio of the level of CIP2A to actin. Data are mean ± SD. n = 3 for the different time intervals. p-EGFR / p-IGF1R / p-ERK / p-AKT; PubMed: 26052929 Mol Carcinog Effects of afatinib on EGFR and IGF1R Signaling Pathways. H1975 cells were treated with afatinib with various doses and cell lysates were subjected to Western blot analysis. Afatinib effectively inhibits p-EGFR and p-ERK while p-AKT was partially inhibited. IGF1R phosphorylation was increased upon afatinib treatment in H1975 cells.	25537503 26052929
Immunofluorescence	p65 ; PubMed: 26317651 Oncotarget Effects of different treatments on the nuclear translocation of the NF-κB subunit p65. A2780T cells were treated with 2.5 μM afatinib for 48 hours, or 10 μM PDTC for 2 hours. Subsequently, the NF-κB subunit p65 (red) was localized by immunofluorescence and a confocal microscopy. Nuclei were stained with DAPI (blue). Scale bar = 10 μm. vacuoles; PubMed: 29713246 Cancer Cell Int Autophagy activation upon treatment with Afatinib and Sorafenib was validated using immunofluorescence in order to visualize a creation of autophagosomes; ×60 magnification. DMSO treatment was used as control. Green—autophagy vacuoles; Blue—Hoechst, nuclear staining.	26317651 29713246

In vivo

In the MDA-MB-453 xenograft model, BIBW2992 (20 mg/kg, p.o.) results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%, and downregulation of EGFR and AKT phosphorylation.^[1] In A7, A431, FaDu, UT-SCC-14 and UT-SCC-15 xenograft models, application of BIBW 2992 (30 mg/kg, p.o.) leads to a significant prolongation of tumour growth time.^[3] In HER2-amplified xenograft medel, Afatinib (30 mg/kg, p.o.) results a markedly inhibition in tumor growth and a significant improvement in the duration of overall survival.^[4] In HER2-positive gastric cancer NCI-N87 xenograft, afatinib (25 mg/kg, p.o.) leads to dramatic tumor volume regression within 4 d and near-complete tumor resolution after 21 d of treatment.^[5]

Protocol

Kinase Assay:^[1]	- Collapse In vitro kinase activity assay: EGFR kinase: Each 100 µL enzyme reaction contained 10 μL of inhibitor in 50% Me2SO, 20 μL of substrate solution (200 mM HEPES pH 7.4, 50 mM Mg-acetate, 2.5 mg/mL poly (EY), 5 μg/mL bio-pEY) and 20 µL enzyme preparation. The enzymatic reaction is started by addition of 50 µL of a 100 µM ATP solution made in 10 mM MgCl2. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 µL of stop solution (250 mM EDTA in 20 mM HEPES pH 7.4). 100 µL are transferred to a streptavidin coated microtiterplate, after an incubation time of 60 min at room temperature the plate is washed with 200 µL of wash solution (50 mM Tris, 0.05% Tween20). A 100 µL aliquot of a HRPO- labeled anti-PY antibody (PY20H Anti-Ptyr:HRP ) 250 ng/mL are added to the wells. After 60 min of incubation, the plate is washed three times with a 200 µL wash solution. The samples are then developed with a 100µL TMB Peroxidase Solution (A:B= 1:1). The reaction is stopped after 10 min. The plate is transferred to an ELISA reader and extinction is measured at OD450nm. HER2-IC enzyme: Enzyme activity is assayed in the presence or absence of serial inhibitor dilutions performed in 50 % Me2SO. Each 100 µL reaction contains similar components as described for EGFR kinase assay with addition of 1000 µM Na3VO4. The enzymatic reaction is started by addition of 50µL of 500 µM ATP solution made in 10 mM Mg-acetate. The dilution of the enzyme is set so that incorporation of phosphate into bio-pEY is linear with respect to time and amount of enzyme. The enzyme preparation is diluted in 20 mM HEPES pH 7.4, 130 mM NaCl, 0.05% Triton X-100, 1 mM DTT and 10% glycerol. Assays are carried out at room temperature for 30 min and terminated by the addition of 50 µL of stop solution. Src kinase assays: Each 100 µL reaction contained 10 µL of inhibitor in 50 % Me2SO, 20µL of enzyme preparation, 20 µL of substrate solution supplemented with 1000 µM Na3VO4. The enzymatic reaction is started by addition of 50 µL of a 1000 µM ATP solution made in 10 mM Mg-acetate. BIRK kinase assay: 250 mM Tris pH 7.4, 10mM DTT, 2.5 mg/mL poly(EY), 5 mg/mL bio-pEY is used as substrate solution and enzymatic reaction is started by addition of 50 µL of a 2 mM ATP solution made in 8 mM MnCl2, 20 mM Mg-acetate. VEGF2 and HGFR kinase assays: Assays are carried out at room temperature for 20 minutes and terminated by the addition of 10 µL of 5 % H3PO4. The precipitate is then trapped onto GF/B filters using a 96 well filter mate universal harvester. After extensive washing the filter plate is dried for 1 h at 50°C, sealed and incorporated radioactivity is determined by scintillation counting using a TopCount™ or a Microbeta b counter™.
Cell Research:^[2]	- Collapse Cell lines: SP and NSP cell lines Concentrations: 1 μM Incubation Time: 48 h Method: Cytotoxicity is determined using MTT assay. The IC 50 value is deﬁned as the drug concentration resulting in 50% cell death. Both the ﬁtted sigmoidal dose response curve and IC50 are calculated by Bliss method. (Only for Reference)
Animal Research:^[4]	- Collapse Animal Models: SCID mice harbouring ARK2 xenografts Dosages: 25 mg/kg Administration: p.o. (Only for Reference)

References

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Solubility (25°C)

In vitro	DMSO	100 mg/mL (139.43 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5% DMSO+30% PEG 300+ddH2O For best results, use promptly after mixing.	28mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download Afatinib (BIBW2992) Dimaleate SDF

Molecular Weight	717.18
Formula	C₂₄H₂₅ClFN₅O₃.2C₄H₄O₄
CAS No.	850140-73-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	CN(C)CC=CC(=O)NC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)OC4CCOC4.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage

mg/kg

Average weight of animals

Dosing volume per animal

Number of animals

Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)

% DMSO+ % + % Tween 80+ % ddH₂O

Calculate Reset

Calculation results:

Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04497584	Not yet recruiting	Drug: Afatinib + Prednisone	Advanced Squamous Non Small Cell Lung Cancer	University of Texas Southwestern Medical Center	March 1 2021	Phase 2
NCT04413201	Recruiting	Drug: Afatinib\|Drug: Osimertinib	Non-squamous NSCLC	Michael Hopp\|Boehringer Ingelheim\|Johannes Gutenberg University Mainz	September 11 2020	Phase 4
NCT04206787	Recruiting	Drug: Afatinib	Non-squamous Non-Small Cell Lung Cancer	Boehringer Ingelheim	May 20 2020	--
NCT04158947	Recruiting	Drug: Afatinib\|Drug: T-DM1	HER2-positive Breast Cancer\|Brain Metastases	xuexin he\|Second Affiliated Hospital School of Medicine Zhejiang University	May 10 2020	Phase 2
NCT03711422	Unknown status	Drug: Afatinib	Non-small Cell Lung Cancer\|Leptomeningeal Disease\|Central Nervous System Metastases	National Cancer Centre Singapore	October 2018	Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

EGFR Signaling Pathway Map

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Afatinib (BIBW2992)

Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFR^wt, EGFR^L858R, EGFR^L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Osimertinib (AZD9291)

Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.
Lapatinib

Lapatinib (GSK572016), used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib induces ferroptosis and autophagic cell death.
AG-490 (Tyrphostin B42)

AG-490 (Tyrphostin B42, Zinc02557947) is an inhibitor of EGFR with IC50 of 0.1 μM in cell-free assays, 135-fold more selective for EGFR versus ErbB2, also inhibits JAK2 with no activity to Lck, Lyn, Btk, Syk and Src.
Rociletinib (CO-1686)

Rociletinib (CO-1686, AVL-301) is an irreversible, mutant-selective EGFR inhibitor with K_i of 21.5 nM and 303.3 nM for EGFR^L858R/T790M and EGFR^WT in cell-free assays, respectively. Phase 2.

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Afatinib (BIBW2992) Dimaleate