Afatinib

• 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].

• Product Name Alternative:

  BIBW 2992

• UNSPSC:

  12352005

• Hazard Statement:

  H302, H319, H373, H402

• Target:

  Akt; Apoptosis; Autophagy; c-Met/HGFR; EGFR; p38 MAPK

• Type:

  Reference compound

• Related Pathways:

  Apoptosis; Autophagy; JAK/STAT Signaling; MAPK/ERK Pathway; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK

• Applications:

  Cancer-Kinase/protease

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Afatinib.html

• Purity:

  99.93

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• 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

• Molecular Formula:

  C24H25ClFN5O3

• Molecular Weight:

  485.94

• Precautions:

  H302, H319, H373, H402

• References & 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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Scientific Category:

  Reference compound1

• Clinical Information:

  Launched

• Isoform:

  EGFR/ErbB1/HER1; ErbB2/HER2; ErbB3/HER3

• Citation 01:

  ACS Appl Mater Interfaces. 2022 May 25;14 (20) :23152-23163.|Acta Histochem. 2019 Nov;121 (8) :151439.|Acta Neuropathol Commun. 2025 Jun 28;13 (1) :143.|Acta Pharmacol Sin. 2023 Jul;44 (7) :1475-1486.|Adv Ther. 2024 Jul 18.|Bioanalysis. 2018 Sep 1;10 (18) :1511-1523.|Biol Direct. 2025 Jul 2;20 (1) :77.|Biol Methods Protoc. 2025 Feb 13;10 (1) :bpaf012.|Biomaterials. 2022 Oct:289:121800.|Biomed Chromatogr. 2016 Jul;30 (7) :1150-4. |bioRxiv. 2023 Sep 13.|bioRxiv. 2024 Feb 12.|bioRxiv. 2024 Jan 4:2023.10.06.561161.|bioRxiv. 2024 October 04.|bioRxiv. 2025 Jun 7:2025.06.04.657911.|bioRxiv. 2025 Nov 24.|bioRxiv. October 28, 2021.|Cancer Cell. 2023 Jan 9;41 (1) :88-105.e8.|Cancer Cell. 2024 Jul 8;42 (7) :1286-1300.e8.|Cancer Discov. 2025 Feb 7;15 (2) :346-362.|Cancer Lett. 2025 Apr 10:217715.|Cancer Nanotechnol. 12, 13 (2021) .|Cancer Res. 2021 Sep 15;81 (18) :4822-4834.|Cancer Res. 2025 Jun 10:10.1158/0008-5472.CAN-24-3904.|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 Feb 21;4 (2) :100911.|Cell Rep Med. 2025 Apr 2:102053.|Chem Eng J. 2024 May 15, 488, 150822.|Cryobiology. 2019 Feb:86:71-76.|EMBO Mol Med. 2021 Apr 9;13 (4) :e13144.|Eur J Drug Metab Pharmacokinet. 2021 Sep;46 (5) :625-635.|Eur J Pharmacol. 2023 Dec 5:960:176114.|Exp Cell Res. 2020 Aug 1;393 (1) :112054.|Fundam Clin Pharmacol. 2021 Oct;35 (5) :919-929.|GEN Biotechnol. 2025 Apr 17.|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 Exp Clin Cancer Res. 2025 Aug 19;44 (1) :245.|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.|Mol Cancer Ther. 2025 Oct 23.|Mol Cell. 2025 Apr 3;85 (7) :1311-1329.e16.|Nat Cell Biol. 2025 Mar;27 (3) :449-463.|Nat Commun. 2025 Feb 1;16 (1) :1237.|Nat Commun. 2025 Nov 23;16 (1) :11115.|Nat Commun. 2019 Apr 18;10 (1) :1812|Nat Genet. 2025 Jan;57 (1) :165-179.|Nature. 2025 Nov 26.|NPJ Parkinsons Dis. 2025 Jun 7;11 (1) :157.|Oncogene. 2018 Aug;37 (31) :4300-4312. |Oncogene. 2022 Aug;41 (32) :3953-3968.|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 Jun;30 (6) :862-874.|Patent. US20190010159A1.|Patent. US20240344020A1|Patent. US20240344020A1.|Pharmaceutics. 2022 Jan 12;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.|SSRN. 2025 Jul 4.|State University of New York at Buffalo. 2025.|Toxicology. 2024 Nov 26:154018.|University of Cádiz. 2023 Oct.|Viruses. 2021 Jun 28;13 (7) :1255.|World J Exp Med. 2025 Jun 20;15 (2) :100443.|Xenobiotica. 2018 Oct;48 (10) :1059-1071. |bioRxiv. 2025 May 9:2025.05.04.652129.|Chem Rep. 2019, 1 (1) : 3-12.|SSRN. 2025 Sep 25.

• CAS Number:

  850140-72-6