AG-1478 (CAS: 153436-53-4) is a reversible and selective inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR). This small molecule inhibitor has shown potential antitumor activity in preclinical studies, making it a promising candidate for cancer therapy.
Chemical name: AG-1478 is also known as N-(3-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine.
Molecular formula: The molecular formula of AG-1478 is C16H14ClN3O2.
Formula weight: Its molecular weight is 315.75 g/mol.
CAS No: The CAS number of AG-1478 is 153436-53-4.
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Synonyms: AG-1478 is also known as Tyrphostin AG-1478 or NSC 693255.
Health benefits of this product: AG-1478 has been shown to inhibit the growth of various tumor types, including breast, lung, ovarian, and head and neck cancers. This compound works by selectively blocking the activation of EGFR, which is frequently overexpressed or mutated in these cancer types. In preclinical studies, AG-1478 has demonstrated potent antitumor activity, indicating that it may be an effective therapeutic option for cancer patients.
Potential effects: AG-1478 has the potential to induce apoptosis (programmed cell death) in cancer cells, thereby inhibiting their growth and proliferation. Additionally, this compound may prevent downstream signaling pathways involved in cell proliferation, survival, migration, and angiogenesis, ultimately leading to tumor growth inhibition.
Product mechanism: AG-1478 selectively targets and binds to the ATP-binding pocket of EGFR, preventing its activation by extracellular ligands. This mechanism of action inhibits downstream signaling pathways involved in cell proliferation, survival, migration, and angiogenesis, ultimately leading to tumor growth inhibition.
Safety: In preclinical studies, AG-1478 has shown a favorable safety profile, with no dose-limiting toxicities observed up to the highest tested doses. However, further studies are required to determine the long-term safety and tolerability of this compound in humans.
Side effects: Common side effects of EGFR inhibitors include diarrhea, rash, fatigue, and nausea. More serious side effects may include hypertension, pneumonitis, and cardiac toxicity.
Dosing information: The optimal dosing regimen for AG-1478 has not yet been established, as this compound is still in the early stages of clinical development. However, preclinical studies have suggested that daily oral administration of 20-100 mg/kg may be an effective dose for inhibiting tumor growth in mouse models.
Conclusion: AG-1478 is a reversible and selective EGFR inhibitor with promising antitumor activity in preclinical studies. This small molecule inhibitor may represent a valuable therapeutic option for cancer patients whose tumors have aberrant EGFR signaling. However, further studies are needed to determine its safety, efficacy, and optimal dosing regimen in humans.
