Afatinib (oxalate)

Afatinib (BIBW 2992) oxalate 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 oxalate 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

[1398312-64-5]

Product Name Alternative

BIBW 2992 (oxalate)

UNSPSC

12352005

Target

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

Type

Reference compound

Related Pathways

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

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/afatinib-oxalate.html

Solubility

10 mM in DMSO

Smiles

OC(C(O)=O)=O.CN(C)C/C=C/C(NC1=CC(C(NC2=CC(Cl)=C(C=C2)F)=NC=N3)=C3C=C1O[C@H]4CCOC4)=O

Molecular Formula

C26H27ClFN5O7

Molecular Weight

575.97

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.