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Erlotinib

产品编号 T0373Cas号 183321-74-6
别名 OSI-744, 埃罗替尼, NSC 718781, CP358774, R1415

Erlotinib (CP358774) 是一种 EGFR 一代抑制剂,抑制 EGFR 19 Del 和 L858R 突变。Erlotinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。Erlotinib 用药会产生 EGFR C797S 耐药突变。

Erlotinib

Erlotinib

纯度: 99.98%
产品编号 T0373 别名 OSI-744, 埃罗替尼, NSC 718781, CP358774, R1415Cas号 183321-74-6

Erlotinib (CP358774) 是一种 EGFR 一代抑制剂,抑制 EGFR 19 Del 和 L858R 突变。Erlotinib 具有抗肿瘤活性,用于治疗 EGFR 突变的非小细胞肺癌。Erlotinib 用药会产生 EGFR C797S 耐药突变。

规格价格库存数量
50 mg¥ 298现货
100 mg¥ 418现货
500 mg¥ 671现货
1 mL x 10 mM (in DMSO)¥ 460现货
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纯度:99.98%
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产品介绍

生物活性
产品描述
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.
靶点活性
EGFR:2 nM (cell free)
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]
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].
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].
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].
别名OSI-744, 埃罗替尼, NSC 718781, CP358774, R1415
化学信息
分子量393.44
分子式C22H23N3O4
CAS No.183321-74-6
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 7.2 mg/mL (18.3 mM), Suspension. Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. 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)
溶液配制表
10% DMSO+40% PEG300+5% Tween 80+45% Saline/Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.5417 mL12.7084 mL25.4168 mL127.0842 mL
5 mM0.5083 mL2.5417 mL5.0834 mL25.4168 mL
10 mM0.2542 mL1.2708 mL2.5417 mL12.7084 mL
Ethanol/DMSO
1mg5mg10mg50mg
20 mM0.1271 mL0.6354 mL1.2708 mL6.3542 mL
DMSO
1mg5mg10mg50mg
50 mM0.0508 mL0.2542 mL0.5083 mL2.5417 mL
100 mM0.0254 mL0.1271 mL0.2542 mL1.2708 mL

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

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