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 |
|---|
| Sevabertinib
Sevabertinib is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor with antitumor activity. |
| BPIQ-I
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. |
| HKI-357
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. |
| SJF-1528
SJF-1528 is a potent EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. |
| CH7233163
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
