Erlotinib mesylate

Overview

Erlotinib (CP-358774) mesylate is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib mesylate also acts as a substrate and inhibitor of OATP2B1 , with an IC 50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib mesylate blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib mesylate inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2 , GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib mesylate is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib mesylate can be used in research related to non-small cell lung cancer , gastric cancer , papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis.

Application

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Product Information

• Catalog No.: HY-12008A
• CAS No.: 248594-19-6
• Molecular Formula: C23H27N3O7S
• Molecular Weight: 489.54
• Purity: 99.98%
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source