An inhibitor of EGFR and ErbB2 (IC50s = 0.5 and 14 nM

Afatinib (maleate) – 500 mg

Brand:
Cayman
CAS:
850140-73-7
Storage:
-20
UN-No:
Non-Hazardous - /

Afatinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and ErbB2 (IC50s = 0.5 and 14 nM, respectively).{33871} It increases the cytotoxicity of adriamycin in a concentration-dependent manner in multidrug-resistant A549T lung cancer cells overexpressing P-glycoprotein.{42401} Afatinib (20 mg/kg) reduces tumor growth in ErbB2-amplified NCI-N87 and NUGC4 gastric cancer mouse xenograft models.{42402} Formulations containing afatinib have been used in the treatment of non-small cell lung cancer.  

 

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Description

An inhibitor of EGFR and ErbB2 (IC50s = 0.5 and 14 nM, respectively); increases the cytotoxicity of adriamycin in a concentration-dependent manner in multidrug-resistant A549T lung cancer cells overexpressing P-glycoprotein; reduces tumor growth in ErbB2-amplified NCI-N87 and NUGC4 gastric cancer mouse xenograft models at 20 mg/kg

Formal name: N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2E-butenamide, 2Z-butenedioate (1:2)

Synonyms:  Afatinib dimaleate|BIBW 2992|BIBW 2992MA2

Molecular weight: 718.1

CAS: 850140-73-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|EGFR/ErbB/HER Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Multidrug Resistance

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