Imatinib D8
(Synonyms: 伊马替尼D8,STI571-d8; CGP-57148B-d8) 目录号 : GC39612
Imatinib D8 (STI571 D8) 是 Imatinib (STI571) 的氘代物。Imatinib 是一种口服生物可用的酪氨酸激酶抑制剂，可选择性抑制 BCR/ABL，v-Abl，PDGFR，c-kit 激酶活性。
Cas No.:1092942-82-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Imatinib D8 (STI571 D8) is a deuterium labeled Imatinib (STI571). Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity[1][2].
[1]. Heinrich MC, et al. Inhibition of c-kit receptor tyrosine kinase activity by STI 571, a selective tyrosine kinase inhibitor. Blood. 2000 Aug 1;96(3):925-32. [2]. Guida T, et al. Sorafenib inhibits imatinib-resistant KIT and platelet-derived growth factor receptor beta gatekeeper mutants. Clin Cancer Res. 2007 Jun 1;13(11):3363-9.
| Cas No. | 1092942-82-9 | SDF | |
| 别名 | 伊马替尼D8,STI571-d8; CGP-57148B-d8 | ||
| Canonical SMILES | O=C(NC1=CC=C(C)C(NC2=NC=CC(C3=CC=CN=C3)=N2)=C1)C4=CC=C(CN5C([2H])([2H])C([2H])([2H])N(C)C([2H])([2H])C5([2H])[2H])C=C4 | ||
| 分子式 | C29H23D8N7O | 分子量 | 501.65 |
| 溶解度 | Soluble in DMSO | 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 | 1.9934 mL | 9.9671 mL | 19.9342 mL |
| 5 mM | 0.3987 mL | 1.9934 mL | 3.9868 mL |
| 10 mM | 0.1993 mL | 0.9967 mL | 1.9934 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。
Development and validation of an LC-MS/MS method for the quantification of imatinib and Imatinib-D8 in human plasma for the support of an absolute bioavailability microdose trial
Pharmazie 2020 Apr 6;75(4):136-141.PMID:32295689DOI:10.1691/ph.2020.9150.
Here we describe the development and validation of an LC-MS/MS method for the quantification of imatinib and Imatinib-D8 in plasma for the support of a clinical absolute bioavailability microdosing trial. The focus lies on the technical aspects to analyse high concentrations of imatinib and low concentrations of Imatinib-D8 that are present simultaneously in study samples, using a single sample processing and analytical method. With the validated assay, imatinib and Imatinib-D8 can be quantified simultaneously in ranges from 25.0 - 5,000 ng/mL and 0.01 - 2.0 ng/mL, respectively. The method was successfully applied in an Imatinib-D8 absolute bioavailability microdosing trial, where a 100 μg Imatinib-D8 microdose was intravenously administered to a patient on oral imatinib treatment 400 mg once daily.
Determination of the absolute bioavailability of oral imatinib using a stable isotopically labeled intravenous Imatinib-D8 microdose
Eur J Clin Pharmacol 2020 Aug;76(8):1075-1082.PMID:32430518DOI:10.1007/s00228-020-02888-y.
Purpose: The aim of this study was to ascertain whether the absolute bioavailability of oral imatinib (Glivec®) during steady state plasma pharmacokinetics in cancer patients could be determined through a concomitant intravenous administration of a single 100 μg microdose of deuterium labeled imatinib (Imatinib-D8). Secondly, the usefulness of liquid chromatography-tandem mass spectrometry (LC-MS/MS) was investigated for simultaneous analysis of orally and intravenously administered imatinib. Methods: Included patients were on a stable daily dose of 400 mg oral imatinib prior to study participation. On day 1, patients received a 100 μg intravenous Imatinib-D8 microdose 2.5 h after intake of the oral dose. Plasma samples were collected for 48 h. Imatinib and Imatinib-D8 concentrations were simultaneously quantified using a validated LC-MS/MS assay. The absolute bioavailability was calculated by comparing the dose-normalized exposure with unlabeled and stable isotopically labeled imatinib in plasma. Results: A total of six patients were enrolled. All patients had a history of gastrointestinal stromal tumors (GIST). The median absolute bioavailability of oral imatinib at steady state was 76% (range 44-106%). Imatinib and Imatinib-D8 plasma concentrations were quantified in all collected plasma samples, with no samples below the limit of quantification for Imatinib-D8. Conclusion: The absolute bioavailability of imatinib was successfully estimated at steady state plasma pharmacokinetics using the stable isotopically labeled microdose trial design. This study exhibits the use of a stable isotopically labeled intravenous microdose to determine the absolute bioavailability of an oral anticancer agent in patients with LC-MS/MS as the analytical tool.