Afatinib (Standard)

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

CAS Number

[850140-72-6]

Product Name Alternative

BIBW 2992 (Standard)

UNSPSC

12352005

Hazard Statement

H302, H319, H373, H402

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-standard.html

Purity

97.64

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.