| Name | Afatinib |
| Description | Afatinib (BIBW 2992) is an irreversible inhibitor of the EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M, and HER2) with IC50s of 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively. |
| In vitro | METHODS: NSCLC cells NCI-H1975, NCI-H1781, HCC827 and A549 were treated with Afatinib (0.0001-10 µM) for 72 h. Cell viability was measured by MTS assay.
RESULTS: Afatinib inhibited the survival of tumor cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR. Afatinib is also effective against NSCLC cell lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), but is inactive against A549 cells expressing wild-type EGFR and HER2 but also harboring the oncogenic Kras G12S point mutation. [1]
METHODS: BEAS-2B cells overexpressing wild-type or mutant HER2 were treated with Afatinib (0.1 µM) for 6 h, and target protein expression levels were measured by Western Blot.
RESULTS: Afatinib treatment inhibited the phosphorylation of HER2, EGFR and AKT. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, Afatinib (20 mg/kg, 1.8% HP-beta-CD + 5% acetic acid (10%) + aqueous Natrosol (0.5%)) was administered by gavage to NMRI-nu/nu mice bearing A431 xenografts once daily for 25 days.
RESULTS: Afatinib resulted in significant tumor regression with a cumulative treatment/control tumor volume ratio (T/C ratio) of 2% and downregulation of EGFR and AKT phosphorylation. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 45 mg/mL (92.6 mM)
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| Keywords | NIH-3T3 cells | ESCC | NSCLC | NCI-H1975 | Afatinib | inhibit | ErbB-1 | HKESC-2 | EC-1 | PKB | H1666 | c-Met/HGFR | Apoptosis | SLMT-1 | H3255 | A431 | BIBW-2992 | lung cancer | EGFR | Akt | Inhibitor | BIBW2992 | HER2 | Autophagy | Epidermal growth factor receptor | HKESC-1 | anticancer | Protein kinase B | orally active | p38 MAPK | HER1 |
| Inhibitors Related | Hydroxychloroquine | Guanidine hydrochloride |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Anti-Aging Compound Library | Bioactive Compounds Library Max |
United States
