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Afatinib

Afatinib

Item no.	HY-10261-5mg
Manufacturer	MedChem Express
CASRN	850140-72-6
Amount	5 mg
Quantity options	100 mg 10 mM/1 mL 10 mg 200 mg 50 mg 5 mg
Category	Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Purity	99.93
Citations	[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.\|[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.\|[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.\|[4]Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109(4):1166-1176. ACS Appl Mater Interfaces. 2022 May 12.\|Acta Histochem. 2019 Nov;121(8):151439.\|Acta Pharmacol Sin. 2023 Feb 1.\|Adv Ther. 2024 Jul 18.\|Bioanalysis. 2018 Sep 1;10(18):1511-1523.\|Biol Methods Protoc. 2025 Feb 13.\|Biomaterials. 16 September 2022.\|Biomed Chromatogr. 2016 Jul;30(7):1150-4. \|bioRxiv. 2023 Oct 6.\|bioRxiv. 2023 Sep 13.\|bioRxiv. 2024 Feb 12.\|bioRxiv. 2024 October 04.\|bioRxiv. October 28, 2021.\|Cancer Cell. 2022 Dec 7;S1535-6108(22)00562-1.\|Cancer Cell. 2024 Jul 8;42(7):1286-1300.e8.\|Cancer Discov. 2024 Dec 5.\|Cancer Nanotechnol. 12, 13 (2021).\|Cancer Res. 2021 Sep 15;81(18):4822-4834.\|Cancer Sci. 2018 Apr;109(4):1166-1176.\|Cancers (Basel). 2024 Aug 7;16(16):2785.\|Cell Biol Int. 2020 Feb;44(2):621-629.\|Cell Death Dis. 2021 Jan 7;12(1):42.\|Cell Physiol Biochem. 2018;47(3):1259-1273.\|Cell Rep Med. 2023 Jan 10;100911.\|Chem Eng J. 2024 May 15, 488, 150822.\|Cryobiology. 2019 Feb;86:71-76.\|EMBO Mol Med. 2021 Mar 4;e13144.\|Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11.\|Eur J Pharmacol. 2023 Oct 18:176114.\|Exp Cell Res. 2020 Aug 1;393(1):112054.\|Fundam Clin Pharmacol. 2021 Feb 1.\|Genes (Basel). 2024 Dec 19;15(12):1624.\|Harvard Medical School LINCS LIBRARY\|Int J Radiat Biol. 2021;97(2):170-178.\|J Exp Clin Cancer Res. 2023 Oct 27;42(1):284.\|J Exp Clin Cancer Res. 2024 Nov 20;43(1):308.\|J Hematol Oncol. 2024 Jul 30;17(1):58.\|J Mater Chem B. 2016 Nov 7;4(41):6652-6661.\|J Oral Biosci. 2024 Sep 6:S1349-0079(24)00198-1.\|J Pharm Anal. 2019 Feb;9(1):49-54. \|J Pharm Biomed Anal. 2018 May 30;154:321-331. \|J Transl Med. 2022 Jun 25;20(1):286.\|Mol Cancer Res. 2019 Nov;17(11):2233-2243.\|Mol Cancer Ther. 2018 Mar;17(3):603-613.\|Nat Cell Biol. 2025 Feb 21.\|Nat Commun. 2025 Feb 1;16(1):1237.\|Nat Commun. 2019 Apr 18;10(1):1812\|Oncogene. 2018 Aug;37(31):4300-4312. \|Oncogene. 2022 Jul 7.\|Oncol Lett. 2021 Nov;22(5):754.\|Oncotarget. 2014 Dec 15;5(23):11971-85.\|Oncotarget. 2015 Oct 13;6(31):31313-22. \|Osteoarthritis Cartilage. 2022 Feb 15;S1063-4584(22)00035-8.\|Patent. US20190010159A1.\|Patent. US20240344020A1\|Patent. US20240344020A1.\|Pharmaceutics. 2022, 14(1), 176.\|Pharmacol Res. 2019 Jun;144:79-89. \|Pharmacol Res. 2020 Sep;159:104934.\|PLoS Comput Biol. 2020 Feb 26;16(2):e1007701. \|PLoS One. 2018 Jun 4;13(6):e0198364.\|PLoS One. 2024 Nov 1;19(11):e0308647.\|Research Square Preprint. 2021 Jul.\|Research Square Preprint. 2024 Nov 26.\|Research Square Print. 2023 Jan 6.\|Sci Signal. 2021 Jun 22;14(688):eabe6156.\|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.\|Toxicology. 2024 Nov 26:154018.\|University of Cádiz. 2023 Oct.\|Viruses. 2021 Jun 28;13(7):1255.\|Xenobiotica. 2018 Oct;48(10):1059-1071. \|Chem Rep. 2019, 1(1): 3-12.
Smiles	O=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[C@H]4CCOC4)/C=C/CN(C)C
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	BIBW 2992
Shipping Condition	Room temperature
Available
Manufacturer - Type	Reference compound
Manufacturer - Applications	Cancer-Kinase/protease
Manufacturer - Targets	Akt; Apoptosis; Autophagy; c-Met/HGFR; EGFR; p38 MAPK
Shipping Temperature	Room Temperature
Storage Conditions	-20°C, 3 years; 4°C, 2 years (Powder)
Molecular Weight	485.94
Product Description	Afatinib (BIBW 2992) is an orally active, potent and irreversible dual specificity inhibitor of ErbB family (EGFR and HER2), with IC50 values of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively. Afatinib can be used for the research of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC) and gastric cancer[1][2][3][4].
Manufacturer - Research Area	Cancer
Solubility	DMSO: 100 mg/mL (ultrasonic)
Manufacturer - Pathway	Apoptosis; Autophagy; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK
Isoform	EGFR/ErbB1/HER1; ErbB2/HER2; ErbB3/HER3
Clinical information	Launched

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