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Erlotinib

产品编号 T0373 CAS 183321-74-6

别名: OSI-744, NSC 718781, CP358774, 埃罗替尼, R1415

Erlotinib (NSC-718781) 是一种直接作用的EGFR 酪氨酸激酶抑制剂，用于治疗非小细胞肺癌，对人 EGFR 的IC50为 2 nM。它可降低完整肿瘤细胞的 EGFR 自磷酸化，IC50为 20 nM。

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Erlotinib, CAS 183321-74-6

规格	价格/CNY	货期
50 mg	￥ 298	现货
100 mg	￥ 418	现货
500 mg	￥ 671	现货
1 mL * 10 mM (in DMSO)	￥ 460	现货

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其他形式的 Erlotinib:

选择批次

纯度: 99.98%

纯度: 99.89%

纯度: 98.19%

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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 (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 是一种针对人类EGFR酪氨酸激酶的抑制剂（其IC50为2 nM），能在完整肿瘤细胞中降低EGFR自磷酸化（IC50为20 nM）。Erlotinib 也是重组内源性（激酶）结构域EGFR的强效抑制剂，IC50为1 nM。Erlotinib 还能强烈抑制DiFi细胞的增殖，在8天的增殖实验中IC50为100 nM[1]。
体内活性	与CP+载体(V)组相比，Erlotinib（20 mg/kg, 口服）显著减轻顺铂(CP)诱导的大鼠体重(BW)损失。Erlotinib 治疗显著改善CP-N（正常对照组，NC）大鼠的肾功能。与CP+V组相比，CP+E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)指数均显著减少（P<0.05），尿量(UV)和肌酐清除率(Ccr)显著增加（P<0.05）[2]。Erlotinib 抑制小鼠体内人头颈部癌HN5肿瘤移植瘤的生长，ED50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	OSI-744, NSC 718781, CP358774, 埃罗替尼, R1415
分子量	393.44
分子式	C22H23N3O4
CAS No.	183321-74-6

存储

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

溶解度

DMSO: 72 mg/mL (183 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 12 mg/mL (30.5 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 / Ethanol	1 mM	2.5417 mL	12.7084 mL	25.4168 mL	63.5421 mL
	5 mM	0.5083 mL	2.5417 mL	5.0834 mL	12.7084 mL
	10 mM	0.2542 mL	1.2708 mL	2.5417 mL	6.3542 mL
	20 mM	0.1271 mL	0.6354 mL	1.2708 mL	3.1771 mL
DMSO	50 mM	0.0508 mL	0.2542 mL	0.5083 mL	1.2708 mL
DMSO	100 mM	0.0254 mL	0.1271 mL	0.2542 mL	0.6354 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)

溶液体积

质量

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. 5. Zhang F, Wang W, Long Y, et al. Characterization of drug responses of mini patient-derived xenografts in mice for predicting cancer patient clinical therapeutic response[J]. Cancer Communications. 2018, 38(1): 1-12. 6. Liu A D, Zhou J, Bi X Y, et al. Aptamer‐SH2 superbinder‐based targeted therapy for pancreatic ductal adenocarcinoma[J]. Clinical and Translational Medicine. 2021, 11(3): e337. 7. Luo P, Yan H, Du J, et al. PLK1 (polo like kinase 1)-dependent autophagy facilitates gefitinib-induced hepatotoxicity by degrading COX6A1 (cytochrome c oxidase subunit 6A1)[J]. Autophagy. 2020: 1-17.

文献引用

1. Liu A D, Zhou J, Bi X Y, et al. Aptamer-SH2 superbinder-based targeted therapy for pancreatic ductal adenocarcinoma. Clinical and Translational Medicine. 2021, 11(3): e337 2. Luo P, Yan H, Du J, et al. PLK1 (polo like kinase 1)-dependent autophagy facilitates gefitinib-induced hepatotoxicity by degrading COX6A1 (cytochrome c oxidase subunit 6A1). Autophagy. 2021 Oct;17(10):3221-3237. 3. Liu A D, Zhou J, Bi X Y, et al. Aptamer‐SH2 superbinder‐based targeted therapy for pancreatic ductal adenocarcinoma. Clinical and Translational Medicine. 2021 Mar;11(3):e337. doi: 10.1002/ctm2.337. 4. Li W, Iusuf D, Sparidans R W, et al.Organic anion-transporting polypeptide 2B1 knockout and humanized mice; insights into the handling of bilirubin and drugs.Pharmacological Research.2023: 106724. 5. Pan Q, Xie Y, Zhang Y, et al.EGFR core fucosylation, induced by hepatitis C virus, promotes TRIM40-mediated-RIG-I ubiquitination and suppresses interferon-I antiviral defenses.Nature Communications.2024, 15(1): 652. 6. Liang J, Bi G, Sui Q, et al.Transcription factor ZNF263 enhances EGFR-targeted therapeutic response and reduces residual disease in lung adenocarcinoma.Cell Reports.2024, 43(2).

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 183321-74-6 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR ErbB-1 CP 358774 cancer tumor acting OSI-774 OSI-744 inhibit CP-358774 OSI 774 Inhibitor OSI774 directly NSC-718781 R 1415 intact NSC 718781 HER1 cell autophosphorylation OSI744 R-1415 Epidermal growth factor receptor lung non-small CP358774 OSI 744 埃罗替尼 NSC718781 R1415 inhibitor

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Erlotinib

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

文献引用

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剂量换算

体内实验配液计算器

技术支持

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