Erlotinib Hydrochloride (CAS 183319-69-9) is a first‑generation, reversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor belonging to the quinazolinamine class. The molecule features a quinazoline core with bis(2‑methoxyethoxy) substituents at the 6,7‑positions and an ethynylanilino group at the 4‑position, with the hydrochloride salt formed at the quinazoline nitrogen.
Erlotinib Hydrochloride is a potent, reversible EGFR tyrosine kinase inhibitor that reduces EGFR autophosphorylation in intact tumor cells with an IC₅₀ of 20 nM. As a quinazolinamine derivative, Erlotinib Hydrochloride competitively inhibits ATP binding at the EGFR kinase domain, blocking downstream signaling pathways involved in tumor cell proliferation and survival. The compound is approved for the treatment of non‑small cell lung cancer and pancreatic cancer, with clinical efficacy demonstrated in patients with EGFR‑mutant tumors. Erlotinib Hydrochloride also exhibits multiple polymorphic forms that vary in solubility, stability, and bioavailability, which are crucial considerations for pharmaceutical formulation development. As a high‑purity reference standard, Erlotinib Hydrochloride is indispensable for analytical method development, impurity profiling, quality control testing, and ANDA filings for generic erlotinib manufacturers. Additionally, Erlotinib Hydrochloride serves as a critical tool compound for studying EGFR signaling, drug resistance mechanisms, and developing next‑generation EGFR‑targeted therapies.
Product Parameters
Parameter
Specification
Product Name
Erlotinib Hydrochloride
CAS Number
183319-69-9
Molecular Formula
C₂₂H₂₄ClN₃O₄
Molecular Weight
429.90 g/mol
Appearance
Offwhite to pale yellow solid
Melting Point
223225°C
pKa
5.42 at 25°C
Solubility
DMSO: up to 18 mg/mL with warming
Storage Condition
Inert atmosphere, store in freezer, under −20°C
Antitumor Drugs
Erlotinib Hydrochloride is a small-molecule reversible inhibitor of the epidermal growth factor receptor tyrosine kinase, primarily indicated for second-or third-line treatment of locally advanced or metastatic non-small cell lung cancer and pancreatic cancer.
Mechanism Of Action
Erlotinib hydrochloride selectively and reversibly targets the epidermal growth factor receptor tyrosine kinase subtype (EGFR-TK). Its mechanism of action involves competing with substrates intracellularly to inhibit EGFR-TK phosphorylation, thereby blocking tumor cell signaling pathways, suppressing tumor growth, and inducing apoptosis. Clinical studies have demonstrated its inhibitory effects against various tumors, offering advantages over conventional chemotherapeutic agents such as milder adverse reactions, improved safety profiles, and better tolerability.
Application
1. Erlotinib Hydrochloride is a small-molecule reversible inhibitor of the epidermal growth factor receptor tyrosine kinase, primarily indicated for second-or third-line treatment of locally advanced or metastatic non-small cell lung cancer and pancreatic cancer.
2. HER-1/EGFR tyrosine kinase inhibitors.
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