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产品介绍
产品介绍
产品信息
抗原名称
EGFR
商品描述
Erlotinib (厄洛替尼; OSI-744; NSC 718781; R1415) 是EGFR抑制剂，IC50为2 nM，比对人c-Src和v-Abl的抑制性高1000倍以上。
分子量
393.44
纯度
＞99%
可溶性
Ethanol ：12 mg/mL (30.5 mM)
DMSO ：72 mg/mL (183 mM)
DMSO ：72 mg/mL (183 mM)
外观
White to off white Solid
In vitro(体外研究)
Erlotinib HCl potently inhibits EGFR activation in intact cells including HNS human head and neck tumor cells (IC50 20nM), DiFi human colon cancer cells and MDA MB-468 human breast cancer cells. Erlotinib HCl (1 μM) induces apoptosis in DiFi human colon 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.
In vivo(体内研究)
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. Erlotinib HCl (100 mg/Kg) inhibits H460a and A549 tumor models with 71 and 93% inhibition rate.
背景
别名
厄洛替尼；埃罗替尼
分子式
C22H23N3O4
CAS号
183321-74-6
制备和贮存
保存方式
Store at -20℃ for three years（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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