All AbMole products are for research use only, cannot be used for human consumption.
In vitro: BIBW2992 is more effective than erlotinib, gefitinib, or lapatinib in inhibiting survival of lung cancer cell lines harboring wild-type (H1666) or L858R/T790M (NCI-H1975) EGFR. BIBW2992 is similarly effective against NSCLC lines expressing HER2 776insV (NCI-H1781) or EGFR E746_A750del (HCC827), but shows no activity toward A549 cells, which express wild-type EGFR and HER2. Afatinib enhances cytotoxicity of topotecan and mitoxantrone to SP cells, and increases the apoptosis induced by topotecan and mitoxantrone in SP cells. In vivo: In the MDA-MB-453 xenograft model, BIBW2992 (20 mg/kg, p.o.) results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%, and downregulation of EGFR and AKT phosphorylation. In A7, A431, FaDu, UT-SCC-14 and UT-SCC-15 xenograft models, application of BIBW 2992 (30 mg/kg, p.o.) leads to a significant prolongation of tumour growth time. In HER2-amplified xenograft medel, Afatinib (30 mg/kg, p.o.) results a markedly inhibition in tumor growth and a significant improvement in the duration of overall survival. In HER2-positive gastric cancer NCI-N87 xenograft, afatinib (25 mg/kg, p.o.) leads to dramatic tumor volume regression within 4 d and near-complete tumor resolution after 21 d of treatment.
Theranostics. 2020 Aug 29;10(24):10925-10939.
Targeting positive feedback between BASP1 and EGFR as a therapeutic strategy for lung cancer progression
Afatinib dimaleate purchased from AbMole
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Afatinib dimaleate purchased from AbMole
FASEB J. 2018 May 29;fj201800011R.
Resistance to gefitinib and cross-resistance to irreversible EGFR-TKIs mediated by disruption of the Keap1-Nrf2 pathway in human lung cancer cells
Afatinib dimaleate purchased from AbMole
| Molecular Weight | 717.18 |
| Formula | C24H25ClFN5O3.2C4H4O4 |
| CAS Number | 850140-73-7 |
| Solubility (25°C) | 80 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related EGFR/HER2 Products |
|---|
| AEE788
AEE788 (NVP-AEE788) is a novel multitargeted HER 1/2 and VEGFR 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. |
| Sapitinib (AZD8931)
AZD8931 (Sapitinib) is an equipotent, reversible inhibitor of Signaling by EGFR, ERBB2 (HER2), and ERBB3 with IC50 of 4, 3, 4 nM respectively. |
| Afatinib
Afatinib (BIBW 2992) is a novel irreversible dual EGFR and HER2 tyrosine kinase inhibitor. |
| CP-724714
CP-724714 is a potent and selective orally active HER-2 tyrosine kinase inhibitor, IC50 = 3 nM. |
| Erlotinib Hydrochloride
Erlotinib is an inhibitor of human EGFR tyrosine kinase (IC50 = 2 nM) and decreases EGFR autophosphorylation in tumor cells (IC50 = 20 nM). |
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Products are for research use only. Not for human use. We do not sell to patients.
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