Afatinib-d4
Afatinib-d4 is the deuterium labeled Afatinib. Afatinib (BIBW 2992) is an irreversible EGFR family inhibitor with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM for EGFRwt, EGFRL858R, EGFRL858R/T790M and HER2, respectively.
Product Specifications
Product Name Alternative
BIBW 2992-d4
UNSPSC
12352005
Target
Autophagy; EGFR
Type
Isotope-Labeled Compounds
Related Pathways
Autophagy; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK
Field of Research
Cancer
Solubility
10 mM in DMSO
Smiles
O=C(NC1=C(C=C2C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)=C1)O[C@H]4CC([2H])([2H])OC4([2H])[2H])/C=C/CN(C)C
Molecular Formula
C24H21D4ClFN5O3
Molecular Weight
489.96
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]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.|[4]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.|[5]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
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Available Sizes
Frequently Asked Questions
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