Afatinib (dimaleate)

Afatinib (dimaleate)

• CAS Number: 850140-73-7
• UNSPSC Description: Afatinib (BIBW 2992) dimaleate 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 dimaleate 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].
• Target Antigen: 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-dimaleate.html
• Purity: 99.88
• Solubility: DMSO : ≥ 35 mg/mL|H2O : 50 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.O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O
• Molecular Weight: 718.08
• 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.Chem Rep. 2019, 1(1): 3-12.|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.|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 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.|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 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.|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.|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.|University of Cádiz. 2023 Oct.|Viruses. 2021 Jun 28;13(7):1255.|Xenobiotica. 2018 Oct;48(10):1059-1071.
• Shipping Conditions: Room Temperature
• Storage Conditions: 4°C (Powder, sealed storage, away from moisture)
• Clinical Information: Launched