(E/Z) -Afatinib

(E/Z) -Afatinib ((E/Z) -BIBW 2992) is the mixture of (E) -Afatinib and (Z) -Afatinib. Afatinib (HY-10261) is an irreversible inhibitor of EGFR, by irreversibly binding to their ATP binding site to block activation of EGFR, HER2, HER4, and EGFRvIII. Afatinib used in co-administration with Temozolomide (HY-17364), potently targeting to EGFRvIII-cMet signaling in glioblastoma cells[1].

Product Specifications

CAS Number

[439081-18-2]

Product Name Alternative

(E/Z) -BIBW 2992

UNSPSC

12352005

Hazard Statement

H302, H319, H373

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

COVID-19-immunoregulation

Field of Research

Others; Cancer

Assay Protocol

https://www.medchemexpress.com/e-z-afatinib.html

Purity

99.98

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(/C=C/CN(C)C)NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1O[C@@H]4COCC4

Molecular Formula

C24H25ClFN5O3

Molecular Weight

485.94

Precautions

H302, H319, H373

References & Citations

[1]Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109 (4) :1166-1176.|[2]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.|[3]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.|[4]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.