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Erlotinib hydrochloride Usage and Function.

Erlotinib targets the epidermal growth factor receptor subtype (EGFR-TK) that reversibly and selectively acts on tyrosine kinase receptors. Its mechanism of action is to compete with substrates in the cell, inhibit EGFR-TK phosphorylation, block the signaling of tumor cells, inhibit the growth of tumor cells, and induce their apoptosis. Clinical studies have shown that the drug has an inhibitory effect on a variety of tumors. Compared with traditional chemotherapy drugs, it has the advantages of less adverse reactions, better safety and tolerance.

Uses of Erlotinib hydrochloride.

Erlotinib hydrochloride is a small molecule epidermal growth factor receptor tyrosine kinase reversible inhibitor, mainly used in the treatment of locally advanced or metastatic non-small cell lung cancer second or third line treatment and pancreatic cancer.

In vitro study of Erlotinib hydrochloride.

Erlotinib inhibits EGFR autophosphorylation by acting on HNS human head and neck tumor cells, which are cell lines that express high levels of EGFR. Erlotinib had no effect on SBC-5 cell proliferation. In contrast, Erlotinib significantly inhibited the proliferation of PC-9 cells in a dose-dependent manner, and PC-9 cells contained deletion mutations in exon 19 of the EGFR gene. The Erlotinib treatment also did not affect SBC-5 cell migration. Erlotinib inhibited HPAC and Capan-1 cell growth with IC50 of 1.1 and 3µM, respectively. 10 uM Erlotinib inhibits EGFR phosphorylation at Y845 (SRc-dependent phosphorylation) and Y1068(autophosphorylation) sites. Erlotinib acts only on the most sensitive cell lines when it inhibits extracellular signal-regulating kinases, Akt, and S6.

Product Method of Bulk Erlotinib hydrochloride Powder.

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