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Erlotinib hydrochloride

产品编号 T0373L CAS 183319-69-9

别名: 盐酸埃罗替尼, OSI-744, NSC 718781, Erlotinib HCl, CP-358774

Erlotinib hydrochloride (NSC 718781) 抑制EGFR 激酶的IC50为 2 nM，用于治疗非小细胞肺癌。

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Erlotinib hydrochloride Chemical Structure

Erlotinib hydrochloride, CAS 183319-69-9

规格	价格/CNY	货期
50 mg	￥ 298	现货
100 mg	￥ 418	现货
1 g	￥ 820	现货
1 mL * 10 mM (in DMSO)	￥ 460	现货

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其他形式的 Erlotinib hydrochloride:

选择批次

纯度: 99.79%

纯度: 99.52%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Erlotinib hydrochloride (NSC 718781) is an EGFR inhibitor (IC50: 2 nM). It is used for the treatment of non-small cell lung cancer.
靶点活性	EGFR:2 nM (cell free)
体外活性	Erlotinib 是一种直接作用于人类EGFR酪氨酸激酶的抑制剂（IC50为2nM），能够显著降低完整肿瘤细胞中EGFR的自磷酸化作用（IC50为20nM）。同时，Erlotinib 对重组的EGFR细胞内（激酶）域也是一种有效抑制剂（IC50为1nM）。DiFi细胞的增殖受到Erlotinib 的强力抑制，在为期8天的增殖试验中，IC50达到100nM[1]。
体内活性	Erlotinib（20 mg/kg，口服）显著减轻顺铂(CP)所引起的大鼠体重(BW)损失，与CP+载体(V)组相比(P<0.05)。Erlotinib 治疗明显改善了CP-N（正常对照组，NC）大鼠的肾功能。与CP+V大鼠相比，CP+E（Erlotinib ）组大鼠的血清肌酐(s-Cr)水平、血尿素氮(BUN)、尿N-乙酰-β-D-葡萄糖胺酶(NAG)指数显著降低（P<0.05），且尿量(UV)及肌酐清除率(Ccr)显著提高（P<0.05）[2]。Erlotinib 在小鼠体内显著抑制人头颈癌HN5肿瘤异种移植物的生长，ED50值为9 mg/kg [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	盐酸埃罗替尼, OSI-744, NSC 718781, Erlotinib HCl, CP-358774
分子量	429.9
分子式	C22H23N3O4·HCl
CAS No.	183319-69-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 5.5 mg/mL (12.79 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3261 mL	11.6306 mL	23.2612 mL	58.1531 mL
	5 mM	0.4652 mL	2.3261 mL	4.6522 mL	11.6306 mL
	10 mM	0.2326 mL	1.1631 mL	2.3261 mL	5.8153 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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配液浓度

参考文献

1. Moyer JD, et al. Induction of apoptosis and cell cycle arrest by CP-358,774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res. 1997, 57(21), 4838-4848. 2. Wada Y, et al. Epidermal growth factor receptor inhibition with erlotinib partially prevents cisplatin-induced nephrotoxicity in rats. PLoS One. 2014 Nov 12;9(11):e111728. 3. Pollack VA, et al. Inhibition of epidermal growth factor receptor-associated tyrosine phosphorylation in human carcinomas with CP-358,774: dynamics of receptor inhibition in situ and antitumor effects in athymic mice. J Pharmacol Exp Ther. 1999 Nov;291(2):739-48. 4. Li T, et al. Schedule-dependent cytotoxic synergism of pemetrexed and erlotinib in human non-small cell lung cancer cells. Clin Cancer Res. 2007 Jun 1;13(11):3413-22.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Erlotinib hydrochloride 183319-69-9 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR OSI774 Inhibitor HER1 盐酸埃罗替尼 inhibit Epidermal growth factor receptor Erlotinib NSC718781 OSI-744 OSI 744 OSI-774 NSC 718781 OSI744 Erlotinib HCl OSI 774 CP-358774 CP358774 CP 358774 Erlotinib Hydrochloride ErbB-1 NSC-718781 inhibitor

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Erlotinib hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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