Letrozole-d4
(Synonyms: 来曲唑 d4) 目录号 : GC47554
An internal standard for the quantification of letrozole
Cas No.:1133712-96-5
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
Letrozole-d4 is intended for use as an internal standard for the quantification of letrozole by GC- or LC-MS. Letrozole is a potent, cell-permeable inhibitor of aromatase (IC50 = 2 nM).1 It inhibits proliferation of estrogen receptor-positive (ER+) MCF-7 cells when used alone at concentrations ranging from 0.1 to 100 nM and when used at a concentration of 10 nM in combination with testosterone or 4-androstene-3,17-dione.2 It also reduces matrix metalloproteinase-2 (MMP-2) and MMP-9 levels in MCF-7 cells when used at a concentration of 10 nM. Letrozole (10 µg per day) reduces tumor growth in an MCF-7Ca ovariectomized-mouse xenograft model.3 Formulations containing letrozole have been used in the treatment of postmenopausal breast cancer.4
1.Mayhoub, A.S., Marler, L., Kondratyuk, T.P., et al.Optimization of the aromatase inhibitory activities of pyridylthiazole analogues of resveratrolBioorg. Med. Chem.20(7)2427-2434(2012) 2.Mitropoulou, T.N., Tzanakakis, G.N., Kletsas, D., et al.Letrozole as a potent inhibitor of cell proliferation and expression of metalloproteinases (MMP-2 and MMP-9) by human epithelial breast cancer cellsInt. J. Cancer104(2)155-160(2003) 3.Long, B.J., Jelovac, D., Handratta, V., et al.Therapeutic strategies using the aromatase inhibitor letrozole and tamoxifen in a breast cancer modelJ. Natl. Cancer Inst.96(6)456-465(2004) 4.Cohen, M.H., Johnson, J.R., Li, N., et al.Approval summary: Letrozole in the treatment of postmenopausal women with advanced breast cancerClin Cancer Res.8(3)665-669(2002)
| Cas No. | 1133712-96-5 | SDF | |
| 别名 | 来曲唑 d4 | ||
| Canonical SMILES | [2H]C(C([2H])=C(C#N)C([2H])=C1[2H])=C1C(N2C=NC=N2)C3=CC=C(C#N)C=C3 | ||
| 分子式 | C17H7D4N5 | 分子量 | 289.3 |
| 溶解度 | DMF: 16 mg/ml,DMF:PBS (pH 7.2) (1:9): 0.1 mg/ml,DMSO: 16 mg/ml | 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 | 3.4566 mL | 17.2831 mL | 34.5662 mL |
| 5 mM | 0.6913 mL | 3.4566 mL | 6.9132 mL |
| 10 mM | 0.3457 mL | 1.7283 mL | 3.4566 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。
SPE-UPLC-MS/MS assay for determination of letrozole in human plasma and its application to bioequivalence study in healthy postmenopausal Indian women
J Pharm Anal 2016 Aug;6(4):276-281.PMID:29403993DOI:PMC5762604
A rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method is described for determination of letrozole in human plasma. Following solid phase extraction (SPE) of letrozole and Letrozole-d4 on Orochem DVB-LP cartridges, chromatography was performed on Acquity UPLC BEH C18 (50 mm×2.1 mm, 1.7 µm) column using methanol-0.1% formic acid in water (85:15, v/v) as the mobile phase. Detection was carried out on a triple quadrupole mass spectrometer with an electrospray source, operated under positive ionization mode. Quantitation of letrozole and Letrozole-d4 was done using multiple reaction monitoring (MRM) following the transitions at m/z 286.2→217.0 and m/z 290.2→221.0, respectively. The calibration plots were linear through the concentration range of 0.10-100 ng/mL (r2≥0.9990) using 100 µL human plasma. The extraction recovery of letrozole ranged from 94.3% to 96.2% and the intra-batch and inter-batch precision was ≤5.2%. The method was successfully applied to a bioequivalence study of letrozole after oral administration of 2.5 mg tablet formulation to 16 healthy postmenopausal Indian women. The assay reproducibility was also established through incurred sample reanalysis (ISR) of 74 subject samples.