埃罗替尼|T0373

Erlotinib
183321-74-6

￥418 100mg 起订

￥298 50mg 起订

￥671 500mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 埃罗替尼

英文名称：: Erlotinib

CAS号：: 183321-74-6

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.98%

产品类别：: 抑制剂

货号：: T0373

Product Introduction

Bioactivity

名称	Erlotinib
描述	Erlotinib (CP358774) is a first-generation EGFR inhibitor that inhibits the EGFR 19 Del and L858R mutations. Erlotinib has antitumor activity and is used for the treatment of EGFR-mutated non-small-cell lung cancers. Erlotinib administration results in the development of the EGFR C797S resistance mutation.
细胞实验	Exponentially growing cells are seeded in 96-well plastic plates and exposed to serial dilutions of erlotinib (30 nM-20 μM), pemetrexed, or the combination at a constant concentration ratio of 4:1 in triplicates for 72 h. Cell viability is assayed by cell count and the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Growth inhibition is expressed as the percentage of surviving cells in drug-treated versus PBS-treated control cells (which is considered as 100% viability). The IC50 value is the concentration resulting in 50% cell growth inhibition by a 72-h exposure to the drug(s) compared with untreated control cells and is calculated by the CalcuSyn software [4].
激酶实验	96-well plates are coated by incubation overnight at 37 °C with 100 μL per well of 0.25 mg/mL PGT in PBS. Excess PGT is removed by aspiration, and the plate is washed 3 times with washing buffer (0.1% Tween 20 in PBS). The kinase reaction is performed in 50 μL of 50 mM HEPES (pH 7.3), containing 125 mM sodium chloride, 24 mM magnesium chloride, 0.1 mM sodium orthovanadate, 20 μM ATP, 1.6 μg/mL EGF, and 15 ng of EGFR, affinity purified from A431 cell membranes. Erlotinib HCl in DMSO is added to give a final DMSO concentration of 2.5%. Phosphorylation is initiated by addition of ATP and proceeded for 8 minutes at room temperature, with constant shaking. The kinase reaction is terminated by aspiration of the reaction mixture and is washed 4 times with washing buffer. Phosphorylated PGT is measured by 25 minutes of incubation with 50 μL per well HRP-conjugated PY54 anti-phosphotyrosine antibody, diluted to 0.2 μg/mL in blocking buffer (3% BSA and 0.05% Tween 20 in PBS). The antibody is removed by aspiration, and the plate is washed 4 times with washing buffer. The colorimetric signal is developed by addition of TMB Microwell Peroxidase Substrate, 50μL per well, and stopped by the addition of 0.09 M sulfuric acid, 50 μL per well. Phosphotyrosine is estimated by measurement of absorbance at 450 nm. The signal for controls is typically 0.6-1.2 absorbance units, with essentially no background in wells without AlP, EGFR, or PGT and is proportional to the time of incubation for 10 minutes [1].
动物实验	Six-week-old male SD rats weighing 180 to 210 g are used. Cisplatin (CP) is freshly prepared in saline at a concentration of 1 mg/mL and then injected intraperitoneally in SD rats (n=28) at a dose of 7 mg/kg on day 0. To investigate the effect of Erlotinib, 28 CP-N rats are divided into two groups. Separate groups (n=14) each of animals are administered with either Erlotinib (20 mg/kg) (CP+E, n=14) or vehicle (CP+V, n=14) daily by oral gavage from the day -1 (24 hours prior to the CP injection) to day 3. Vehicle-treated groups receive an equivalent volume of saline. Five male SD rats at the age of 6 weeks are used as a normal control group (NC, n=5). The NC rats are given an equivalent volume of saline daily by oral gavage from the day -1 to day 3. At day 4 (96 hours after CP injection), each rat is anesthetized and sacrificed by exsanguination after the cardiac puncture; blood is collected by cardiac puncture and kidneys are collected. Renal tissue is divided; separate portions are snap-frozen in liquid nitrogen or fixed in 2% paraformaldehyde/phosphate-buffered saline (PBS) for later use. All surgery is performed under diethyl ether gas anesthesia, and all efforts are made to minimize suffering [2].
体外活性	方法：人非小细胞肺癌细胞 PC9 用 Erlotinib (0.0002-2 µM) 处理 72 h，检测细胞生存曲线。结果：Erlotinib 抑制 PC9细胞生长，IC50 为 30 nM。[1] 方法：人头颈癌细胞 HN5 用 Erlotinib (20-1000 nM) 处理 1 h，随后用 EGF (50 ng/mL) 刺激 5 min，使用 Western Blot 检测靶点蛋白表达水平。结果：Erlotinib 抑制人头颈部肿瘤细胞中 EGFR 自磷酸化。[2]
体内活性	方法：为测试体内抗肿瘤活性，将 Erlotinib (2.9-92 mg/kg，sterile+pyrogen-free 10% DMSO+0.85% sodium chloride+0.1% Pluronic P105) 灌胃给药给携带人头颈癌肿瘤 HN5 或人鳞状细胞癌肿瘤 A431 的 CD-1 nu/nu 小鼠，每天一次，持续二十天。结果：Erlotinib 抑制 HN5 或 A431 的肿瘤生长。[3]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 7.2 mg/mL (18.3 mM), Suspension. Working solution is recommended to be prepared and used immediately. DMSO : 60 mg/mL (152.5 mM) H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : 12 mg/mL (30.5 mM)
关键字	ErbB-1 \| CP 358774 \| cancer \| tumor \| acting \| OSI-774 \| inhibit \| CP-358774 \| OSI 774 \| Inhibitor \| EGFR \| Autophagy \| Erlotinib \| OSI774 \| directly \| NSC-718781 \| R 1415 \| intact \| HER1 \| cell \| autophosphorylation \| OSI744 \| R-1415 \| Epidermal growth factor receptor \| lung \| non-small \| OSI 744 \| NSC718781
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OSI-744|||埃罗替尼|||NSC 718781|||CP358774|||R1415|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
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