Afatinib (dimaleate) (Standard)

Afatinib (dimaleate) (Standard) is the analytical standard of Afatinib (dimaleate) . This product is intended for research and analytical applications. 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].

Product Specifications

CAS Number

[850140-73-7]

Product Name Alternative

BIBW 2992MA2 (Standard)

UNSPSC

12352005

Target

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

Type

Reference compound

Related Pathways

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

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/afatinib-dimaleate-standard.html

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 Formula

C32H33ClFN5O11

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.