Erlotinib,183321-74-6

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YZ剂描述：

产品名称：Erlotinib

产品别名：厄洛替尼

英文别名：OSI-744;NSC 718781;R1415)

靶点：EGFR

CAS：183321-74-6

纯度：98%

外观：见爱必信官网

保存方法：-20℃冷藏长期储存。冰袋运输

描述：

Erlotinib (厄洛替尼; OSI-744; NSC 718781; R1415) 是EGFRYZ剂，IC50为2 nM，比对人c-Src和v-Abl的YZ性高1000倍以上。

溶解性：Ethanol ：12 mg/mL (30.5 mM)
DMSO ：72 mg/mL (183 mM)

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.

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.

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