 COA |
MSDS |
 HPLC |
NMR |
| CAS No: | 183319-69-9 |
| Molecular formula(MF) | C22H23N3O4.HCl |
| Molecular Weight(MW): | 429.90 |
| Alias | ERLOTINIB; ERLOTINIB HCL SALT; TARCEVA; ERLOTINIB HCL SALT :TARCEVA; Erlotinib, Hydrochloride Salt; N-(3-Ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-; quinazolinamine, Hydrochloride Salt, OSI 774, Tarceva; N-(3-Ethynylphenyl)-6,7-bis-(2-methoxyethoxy)-quinazolin-4-amine; [6,7-Bis-(2-methoxy-ethoxy)-quinazolin-4yl]-(3-ethynyl-phenyl)-amine; Tarceva Hydrochloride See E625000; Erlotinib HCl |
| In vitro | DMSO | 4 mg/mL warmed (9.3 mM) |
|---|---|---|
| Water | <1 mg/mL | |
| Ethanol | <1 mg/mL | |
| In vivo | 15% Captisol | 16 mg/mL warmed |
| Description | Erlotinib HCl (OSI-744) is an EGFR inhibitor with IC50 of 2 nM in cell-free assays, >1000-fold more sensitive for EGFR than human c-Src or v-Abl. | |||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Targets |
|
|||||||||||||||||||||||
| In vitro |
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. [1] 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. [2] Erlotinib HCl(2 μM) significantly inhibits growth of AsPC-1 and BxPC-3 pancreatic cells. [3] 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. [4] Combination with Erlotinib HCl could down-modulate rapamycin-stimulated Akt activity and produces a synergistic effect on cell growth inhibition. [5] |
|||||||||||||||||||||||
| Cell Data |
|
|||||||||||||||||||||||
| In vivo | At doses of 100 mg/kg, Erlotinib HCl completely prevents EGF-induced autophosphorylation of EGFR in human HN5 tumors growing as xenografts in athymic mice and of the hepatic EGFR of the treated mice. [1] Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate. [5] |