Molecular Formula: C32H33ClFN5O11 (alternatively, C28H29ClFN5O7, but C32H33ClFN5O11 is more commonly reported)
Molecular Weight: 718.083 (alternatively, 602.02, but 718.083 is more accurate)
Physical and Chemical Properties
Appearance: Usually appears as a white or nearly white powder.
Solubility: Soluble in organic solvents such as DMSO.
Storage Conditions: Recommended to store at -25-15°C with a shelf life of 3 years. Once dissolved in a solvent, it should be stored at -85-65°C with a shelf life of 2 years. Store in a dark and dry place, avoiding repeated freeze-thaw cycles.
Biological Properties
Targets: Afatinib Dimaleate is an irreversible EGFR family inhibitor, primarily targeting EGFRwt, EGFRL858R, EGFRL858R/T790M, and HER2.
IC50 Values: The IC50 values for EGFRwt, EGFRL858R, EGFRL858R/T790M, and HER2 are 0.5 nM, 0.4 nM, 10 nM, and 14 nM, respectively.
Mechanism of Action: By inhibiting the activity of EGFR and HER2, it blocks the signaling pathways of tumor cells, thereby inhibiting their proliferation and growth.
In Vivo and In Vitro Studies: In vivo studies have shown that Afatinib Dimaleate significantly inhibits tumor growth with low toxicity and good drug tolerance. In vitro studies have demonstrated its significant inhibitory activity against various tumor cell lines.
Applications and Precautions
Applications: Primarily used for scientific research or drug certification applications, especially in the fields of esophageal squamous cell carcinoma (ESCC), non-small cell lung cancer (NSCLC), and gastric cancer.
Precautions: Afatinib Dimaleate is intended for research purposes only and must not be used on humans. During use, wear laboratory coats and disposable gloves, and avoid inhalation, ingestion, or direct contact with skin and eyes.
