Afatinib-d6 dimaleate
Afatinib-d6 (dimaleate) is the deuterium labeled Afatinib dimaleate. Afatinib dimaleate 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.
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- 화학식: C32H27D6ClFN5O11
- 분자량:724.12
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled CAS 850140-73-7
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분자량 724.12
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화학식 C32H27D6ClFN5O11
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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([2H])([2H])[2H])C([2H])([2H])[2H].O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O
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Synonyms
BIBW 2992MA2-d6
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[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. [Content Brief]
[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 [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)