Erlotinib-d6 (hydrochloride)
(Synonyms: 埃罗替尼-D6盐酸盐,CP-358774-d6 hydrochloride; NSC 718781-d6 hydrochloride; OSI-774-d6 hydrochloride) 目录号 : GC47303
An internal standard for the quantification of erlotinib
Cas No.:1189953-78-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Erlotinib-d6 (hydrochloride) contains six deuterium atoms located on the methoxy group. It is intended for use as an internal standard for the quantification of erlotinib by GC- or LC-MS. Erlotinib is a tyrosine kinase inhibitor that acts on the epidermal growth factor receptor (EGFR), inhibiting EGFR-associated kinase activity (IC50 = 2.5 µM).1,2 This inhibits tumor growth in human head and neck carcinoma (HN5) tumor xenografts in mice with an ED50 value of 9 mg/kg.1 Erlotinib also suppresses cyclin-dependent kinase 2 (Cdk2) activity in breast cancer cells (IC50 = 4.6 µM) and JAK2 mutant JAK2V617F (IC50 = 5 µM), which is associated with polycythemia vera, idiopathic myelofibrosis, and essential thrombocythemia.3,4 Formulations containing erlotinib are used to treat certain forms of cancer, including non-small cell lung cancer.5,6
1.Ciardiello, F., and Tortora, G.A novel approach in the treatment of cancer: Targeting the epidermal growth factor receptorClin. Cancer Res.7(10)2958-2970(2001) 2.Greulich, H., Chen, T.H., Feng, W., et al.Oncogenic transformation by inhibitor-sensitive and -resistant EGFR mutantsPLoS Med.2(11)(2005) 3.Yamasaki, F., Zhang, D., Bartholomeusz, C., et al.Sensitivity of breast cancer cells to erlotinib depends on cyclin-dependent kinase 2 activityMol. Cancer Ther.6(8)2168-2177(2007) 4.Li, Z., Xu, M., Xing, S., et al.Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growthJ. Biol. Chem.282(6)3428-3432(2007) 5.Herbst, R.S., and Bunn, P.A., Jr.Targeting the epidermal growth factor receptor in non-small cell lung cancerClin. Cancer Res.9(16)5813-5824(2003) 6.Gerber, D.E.EGFR inhibition in the treatment of non-small cell lung cancerDrug Dev. Res.69(6)359-372(2008)
| Cas No. | 1189953-78-3 | SDF | |
| 别名 | 埃罗替尼-D6盐酸盐,CP-358774-d6 hydrochloride; NSC 718781-d6 hydrochloride; OSI-774-d6 hydrochloride | ||
| Canonical SMILES | C#CC1=CC(NC2=NC=NC3=CC(OCCOC([2H])([2H])[2H])=C(OCCOC([2H])([2H])[2H])C=C32)=CC=C1.Cl | ||
| 分子式 | C22H17D6N3O4.HCl | 分子量 | 435.9 |
| 溶解度 | DMSO: slightly, heated,Methanol: slightly soluble | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2941 mL | 11.4705 mL | 22.941 mL |
| 5 mM | 0.4588 mL | 2.2941 mL | 4.5882 mL |
| 10 mM | 0.2294 mL | 1.1471 mL | 2.2941 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
The Effect of Single-Dose Ougan Juice Application on the Pharmacokinetics of Erlotinib
Biomed Res Int 2021 Jun 11;2021:6679082.PMID:34195278DOI:10.1155/2021/6679082.
The aim of our study was to investigate the effects of single-dose Ougan (Citrus reticulata cv. Suavissima) juice application on the pharmacokinetics of erlotinib in vivo. Twelve Sprague-Dawley rats were randomly divided into the Ougan juice and control groups (n = 6 each). The rats were given a single dose of 1 mL/100 g Ougan juice or 1 mL/100 g normal saline (NS) by intragastric administration, followed by a single oral administration of 20 mg/kg erlotinib. The plasma concentration of erlotinib in rats was determined using ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS). Erlotinib-d6 was used as the internal standard for chromatographic analysis on the UPLC BEH C18 analysis column (2.1 mm × 50 mm, 1.7 μm). The mobile phase was composed of acetonitrile and 0.1% formic acid eluting by gradient. Different pharmacokinetic (PK) parameters of erlotinib were calculated. The Ougan juice promoted the absorption of erlotinib and reduced the clearance of the drug. The area under the curve of erlotinib in the single-dose Ougan juice pretreatment group was approximately 1.87 times higher, and the maximum blood concentration (Cmax) was approximately 1.34 times higher than that in the control group. The mean residence time of erlotinib in the Ougan juice group was larger, and the clearance rate was smaller than those in the control group; the difference was statistically significant (P < 0.05). Ougan juice affected the PK spectrum of erlotinib in rats by improving the bioavailability of the drug and significantly increasing its plasma concentration.
Quantification of the tyrosine kinase inhibitor erlotinib in human scalp hair by liquid chromatography-tandem mass spectrometry: Pitfalls for clinical application
J Pharm Biomed Anal 2019 Aug 5;172:175-182.PMID:31051406DOI:10.1016/j.jpba.2019.04.031.
An LC-MS/MS method was developed and validated to quantify the tyrosine kinase inhibitor erlotinib in human scalp hair, as alternative matrix to monitor long-term erlotinib exposure. Hair samples from 10 lung cancer patients were measured and correlated with plasma concentrations. Hair segments of 1 ± 0.1 cm each were pulverized and for at least 18 h incubated in methanol at ambient temperature. A liquid-liquid extraction purified the extracts and they were analyzed with LC-MS/MS, using Erlotinib-d6 as internal standard. The procedure method was validated for selectivity, sensitivity, precision, lower limit of detection, linearity and accuracy. The within and between run precisions including the lower limit of quantification did not exceed 12.5%, while the accuracy ranged from 103 to 106%. A weak correlation between hair and plasma concentration was found (R2 = 0.48). Furthermore, a large inter-individual variability was noted in the disposition of both plasma and hair samples. The highest hair concentrations were observed in black hair compared with other (grey and brown) hair colors. Generally, a linear reduction in hair concentration was found from proximal to distal hair segments. Additional in vitro experiments suggest an accelerated degradation of erlotinib in hair by artificial UV light and also wash-out by shampoo mixtures pretreatment compared with control samples. In conclusion, a reliable and robust LC-MS/MS method was developed to quantify erlotinib in hair. However, clinical and in vitro evaluations showed that the method is not suitable for monitoring long-term erlotinib exposure. The pitfalls of this application outweigh the current benefits.