ChemicalBook >> CAS DataBase List >>2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)-

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)-

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)- structure

CAS No.: 1398312-64-5

Chemical Name:: 2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)-

Synonyms: Afatinib oxalate;2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)-

CBNumber:: CB213224820

Molecular Formula:: C26H27ClFN5O7

Molecular Weight:: 575.98

MDL Number:

MOL File:: 1398312-64-5.mol

MSDS File:: SDS

Last updated:2026-07-27 17:00:41

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2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)- Chemical Properties, Uses, Production

Uses

Afatinib (BIBW 2992) oxalate is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib oxalate can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer[1][2][3][4].

in vivo

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

Animal Model:	Athymic NMRI-nu/nu female mice (21–31 g, five to six-week-old, transgenic murine lung cancer model and xenograft models)^[1]
Dosage:	15 mg/kg, 20 mg/kg
Administration:	Orally, daily for 25 days
Result:	Resulted in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2% in a standard xenograft model of the epidermoid carcinoma cell line A431, and downregulation of EGFR and AKT phosphorylation. Induced regression of large tumors in this HER2-driven model, effectively controlled xenograft tumor formation by the NCIH1975 cell line, expressing EGFR L858R/T790M, with a T/C value of 12% for doses of 20 mg/kg. Induced more than 50% percent tumor reduction after a 4-week treatment period. Downregulated EGFR, HER2 and HER3 phosphorylation.

Animal Model:	Six weeks old female athymic nude mice (nu/nu) (16-20 g)^[2]
Dosage:	15 mg/kg
Administration:	Oral gavage in a schedule of 5 days on plus 2 days off, for two weeks
Result:	Strongly inhibited the growth of HKESC-2 tumor. Average tumor sizes of vehicle and treatment at end point are 348 ± 24 mm³ and 108 ± 36 mm³ respectively.

IC 50

EGFR^L858R: 0.4 nM (IC₅₀); EGFR^WT: 0.5 nM (IC₅₀); EGFR^L858R/T790M: 10 nM (IC₅₀); HER2: 14 nM (IC₅₀); HER3

References

[1] Li D, et al. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Oncogene. 2008 Aug 7;27(34):4702-11. DOI:10.1038/onc.2008.109
[2] Wong CH, et al. Preclinical evaluation of afatinib (BIBW2992) in esophageal squamous cell carcinoma (ESCC). Am J Cancer Res. 2015 Nov 15;5(12):3588-99. PMID:26885448
[3] Wang XK, et al. Afatinib circumvents multidrug resistance via dually inhibiting ATP binding cassette subfamily G member 2 in vitro and in vivo. Oncotarget. 2014 Dec 15;5(23):11971-85. DOI:10.18632/oncotarget.2647
[4] Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176. DOI:10.1111/cas.13546

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)- Preparation Products And Raw materials

Raw materials

Preparation Products

2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)- Suppliers

Global Suppliers ( 2)

Supplier	Tel	Email	Country	ProdList	Advantage
TargetMol Chemicals Inc.	15002134094	marketing@targetmol.cn	China	29874	58
TargetMol Chemicals Inc.	13564774135	marketing@targetmol.com	United States	19950	58

Supplier	Advantage
TargetMol Chemicals Inc.	58
TargetMol Chemicals Inc.	58

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Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2026-07-27	Afatinib oxalate 1398312-64-5	$2140.00-3520.00			10g	TargetMol Chemicals Inc.

Afatinib oxalate
1398312-64-5
$2140.00-3520.00
TargetMol Chemicals Inc.

1398312-64-5 (2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)-) Related Search:

EGFR Protein, HUMAN (621A.A, HEK293, FC) EGFR protein, HUMAN (BIOTINYLATED, HEK293, HIS-AVI) HER2/CD340 protein, HUMAN (BIOTINYLATED, HEK293, HIS) HER3 Protein, HUMAN (BIOTINYLATED, HEK293, HIS-AVI) EGFR Protein, HUMAN (HEK293, HIS-AVI)

HGFR Protein, Human (HEK293, hFc)

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2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-, ethanedioate (1:2), (2E)- Afatinib oxalate 1398312-64-5 C26H27ClFN5O7