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Tarceva;CP-358774 CP 358774;CP358774;OSI-774;OSI 774;OSI774;NSC-718781;NSC 718781;NSC718781 Erlotinib HCl
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CAS NO. | 183319-69-9 | |
Erlotinib HCl | ||
C22H23N3O4.HCl | ||
429.9 | ||
98% | ||
can supply large quantity in kgs scale | ||
Tarceva;CP-358774;CP 358774;CP358774;OSI-774;OSI 774;OSI774;NSC-718781;NSC 718781;NSC718781 | ||
Erlotinib is a directly acting inhibitor of human EGFR tyrosine kinase with an IC50 of 2 nM. | ||
Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi humancolon cancer cells andMDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi humancolon cancer cells.Erlotinib inhibits growth of a panel of NSCLC cell lines including A549, H322, H3255, H358 H661, H1650, H1975, H1299, H596 with IC50 ranging from 29 nM to >20 μM.Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells.The effects of Erlotinib HCl in combination with gemcitabine are considered additive in KRAS-mutated pancreatic cancer cells. Ten micromolar of Erlotinib HCl inhibits EGFR phospho-rylation at the Y845 (Src-dependent phosphorylation) and Y1068 (auto-phosphorylation) sites. Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. |
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