Bioactivity | Afatinib (BIBW 2992) oxalate 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 oxalate 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]. |
Invitro | Afatinib oxalate (100 nM) sufficiently prevents heregulin-stimulated HER3 phosphorylation[1].Afatinib oxalate (0-10000 nM) effectively inhibits anchorage-independent proliferation of NIH-3T3 cells ectopically expressing EGFR mutants, and inhibits cell proliferation of H1666, H3255, and NCI 1975 cells[1].Afatinib oxalate (48-72 h)shows growth inhibition in HKESC-1, HKESC-2, SLMT-1 and EC-1 cells[2].Afatinib oxalate (0-1 μM, 24-48 h) inhibits AKT and MAPK pathways, and inhibits EGFR and AKT phosphorylation in ESCC cell lines[2].Afatinib oxalate (0-1 μM, 16-48 h) induces G0/G1 cell cycle arrest in HKESC-2 and EC-1[2].Afatinib oxalate (0-1 μM, 24-48 h) effectively induces apoptotic cell death in HKESC-2 and EC-1[2]. Cell Proliferation Assay[1] Cell Line: |
Name | Afatinib oxalate |
CAS | 1398312-64-5 |
Formula | C26H27ClFN5O7 |
Molar Mass | 575.97 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |