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Afatinib (dimaleate) (Standard)

Product Specifications

UNSPSC Description

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].

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

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 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.

Shipping Conditions

Room temperature

Product Datasheet

http://file.medchemexpress.com/batch_PDF/HY-10261AR/Afatinib-dimaleate-Standard-DataSheet-MedChemExpress.pdf

Product MSDS

http://file.medchemexpress.com/batch_PDF/HY-10261AR/

CAS Number

850140-73-7

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