Erlotinib

同義語： Erlotinib, Tarceva, OSI-774, CP-358774, NSC 718781, N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine

Erlotinib is a small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) that has become a cornerstone in the targeted therapy of non-small cell lung cancer (NSCLC) and pancreatic cancer. It belongs to the quinazoline class and works by reversibly binding to the ATP pocket of the EGFR kinase domain, blocking autophosphorylation and downstream signaling. First approved by the FDA in 2004 for advanced NSCLC, erlotinib continues to be a vital tool in precision oncology, particularly for patients with EGFR exon 19 deletions or exon 21 L858R mutations.

Chemically, erlotinib is characterized by a quinazoline core substituted with a 3-ethynylphenylamino group at the 4-position and two 2-methoxyethoxy chains at the 6- and 7-positions. This structure confers high selectivity for EGFR over other kinases and good oral bioavailability. The compound is typically supplied as the hydrochloride salt for pharmaceutical formulations, though the free base is also available for research purposes. Its molecular formula is C22H23N3O4, with a molecular weight of 393.44 g/mol.

As an API, erlotinib is produced under strict cGMP conditions and is available in high purity grades suitable for clinical and commercial manufacturing. It is widely used in the development of generic Tarceva, fixed-dose combinations, and novel formulations. Its reliable pharmacokinetic profile and well-established safety data make it a preferred choice for both innovator and generic pharmaceutical companies.

Function & Mechanism

• EGFR inhibition: Reversibly binds to the ATP-binding site of EGFR, blocking tyrosine kinase activity and downstream proliferation signals.
• Antiproliferative effect: Inhibits cancer cell growth and induces apoptosis in EGFR-mutant tumors.
• Anti-angiogenesis: Downregulates VEGF expression, reducing tumor vascularization.
• Cell cycle arrest: Induces G1 phase arrest by upregulating p27 and downregulating cyclin D1.
• Overcomes resistance: Active against certain EGFR mutations resistant to first-generation TKIs.

Source & Standardization

• 出典: Synthetic chemical synthesis
• Manufacturing: Multi-step organic synthesis under cGMP
• Standardization: ≥99.0% (HPLC), meeting Ph. Eur. and USP monographs
• Forms: Crystalline powder, hydrochloride salt available
• 用途: Pharmaceutical manufacturing, research, clinical trials

Quality Specifications (QC Tests)

Bulk Supply & Documentation

• 月間処理能力: 50 kg
• リードタイム: 3～5営業日（在庫品）
• ドキュメント: COA, MSDS, TDS, DMF available upon request
• パッケージ: 1 kg, 5 kg, 25 kg drums with double LDPE liners

よくある質問

What is the minimum order quantity (MOQ) for Erlotinib?

Our standard MOQ is 1 kg, but we can accommodate smaller quantities for research and development purposes. Please contact us for custom orders.

What is the delivery time?

For stock items, delivery is 3-5 business days from order confirmation. We ship globally via express couriers.

Do you provide a Certificate of Analysis (COA) and samples?

Yes, we provide a COA for every batch. Samples are available upon request, typically shipped within 1-2 days.

Contact & Ordering Information

• Company: LyvBio Co., Ltd.
• Address: Room 5-0203, Courtyard 205, Lianhu District, Xi’an, Shaanxi, China
• Email: info@lyvbio.com
• Phone: +86-29-65816888

send us your specification for a quotation.