Erlotinib hydrochloride (cas 183319-69-9)
Indications: Suitable for locally advanced or metastatic non-small cell lung cancer (NSCLC) after the failure of at least one chemotherapy regimen in the past.
Pharmacology: Erlotinib is a tyrosine kinase inhibitor of the epidermal growth factor receptor. Erlotinib can compete with ATP to bind the intracellular catalytic region of the epidermal growth factor receptor tyrosine kinase, inhibit phosphorylation, block and inhibit the system’s transmission of intranuclear information, and achieve the effect of preventing tumor growth, controlling cell proliferation, neovascularization, and tumor metastasis.
Compound Information: Erlotinib Hydrochloride
| Category | Details |
|---|---|
| Name | Erlotinib Hydrochloride |
| CAS Number | 183319-69-9 |
| Synonyms | Tarceva; OSI-774; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine hydrochloride |
| EINECS Number | 620-491-0 |
| Molecular Formula | C₂₂H₂₄ClN₃O₄ |
| Molecular Weight | 429.9 g/mol |
| Chemical Properties | |
| – Appearance | Off-white solid |
| – Melting Point | 223–225°C |
| – Storage Temp. | -20°C freezer (inert atmosphere) |
| – Solubility | DMSO (up to 18 mg/mL with warming) |
| – Form | Yellow powder |
| – Color | White to off-white |
| – pKa | 5.42 (25°C) |
| InChIKey | GTTBEUCJPZQMDZ-UHFFFAOYSA-N |
Key Notes:
- Chemical Structure:
- A quinazolinamine derivative with a 3-ethynylphenyl group and two 2-methoxyethoxy substituents.
- The hydrochloride salt enhances water solubility for oral bioavailability.
- Pharmacological Role:
- Selective EGFR tyrosine kinase inhibitor (IC₅₀ = 2 nM), blocking cell proliferation and angiogenesis in cancers.
- Targets NSCLC (non-small cell lung cancer) and pancreatic cancer via EGFR pathway modulation.
- Clinical Use:
- Approved Indications:
- Locally advanced/metastatic NSCLC with EGFR mutations.
- Pancreatic cancer (second-line treatment).
- Dosage: 150 mg/day orally (fasting for 1 hour before/2 hours after meals).
- Approved Indications:
- Safety & Toxicity:
- Common Side Effects: Rash, diarrhea, fatigue, nausea.
- Severe Risks: Interstitial lung disease (ILD), hepatotoxicity, gastrointestinal perforation.
- Supplier Information:
- Pricing: ~$0.5–5/mg (varies by purity and order volume).
Analytical & Handling Guidelines:
- Detection: UV-Vis spectroscopy (λmax = 243 nm in phosphate buffer).
- Stability: Stable for 1 year as supplied; DMSO solutions stored at -20°C for ≤3 months.
sale@pharma-peptides.com
请到「后台-用户-个人资料」中填写个人说明。