计算溶液所需的质量、体积或浓度。
概述
Erlotinib hydrochloride is an antineoplastic drug. It regulates mechanistic target of rapamycin (mTOR) inhibition, epidermal growth factor receptor down-regulation and epidermal interstitial transformation (EMT) suppression. Erlotinib Hydrochloride (CP-358774 Hydrochloride) inhibits purified EGFR kinase with an IC50 of 2 nM.
添加用途：
Erlotinib hydrochloride has been used to activate mitochondrial fragmentation in a human PANC-1 pancreatic cancer cell line.
Information
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. 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
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.
Cell Data
cell lines：
Concentrations：30 nM-20 μM
Incubation Time：72 hours
Powder Purity:≥99%
规格
别名
盐酸厄洛替尼 (OSI-744)
英文别名
CP358774, NSC 718781
规格或纯度
2mM in DMSO
英文名称
Erlotinib HCl (OSI-744)
生化机理
盐酸厄洛替尼（OSI-744、CP358774、NSC 718781）是一种表皮生长因子受体（EGFR）抑制剂，在无细胞实验中的 IC50 值为 2 nM，对 EGFR 的敏感性是人类 c-Src 或 v-Abl 的 1000 倍以上。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
表皮生长因子受体 erbB1 抑制剂
名称和识别符
EC号
620-491-0
分子类型
小分子
Isomeric SMILES
COCCOC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC=CC(=C3)C#C)OCCOC.Cl
关联CAS
NSC Number
718781
MeSH Entry Terms
11C erlotinib;11C-erlotinib;358,774, CP;358774, CP;CP 358,774;CP 358774;CP-358,774;CP-358774;CP358,774;CP358774;erlotinib;erlotinib HCl;erlotinib hydrochloride;HCl, Erlotinib;Hydrochloride, Erlotinib;N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-
分子量
429.9
Reaxy-Rn
8813963
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8813963&ln=
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 75 mg/mL (293.8 mM); Water: 75 mg/mL (293.8 mM); Ethanol: 75 mg/mL warmed with 50ºC Water: bath (293.8 mM);
熔点
228 °C
安全和危险性（GHS）
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403+P235: 存放在通风良好的地方。保持低温。
P501: 将内容物/容器送到批准的废物处理厂处理
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
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危险品化学品经营许可证（带存储）