Fulvestrant-d3
(Synonyms: ICI 182780-d3; ZD 9238-d3; ZM 182780-d3) 目录号 : GC40241
An internal standard for the quantification of fulvestrant
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
Fulvestrant-d3 is intended for use as an internal standard for the quantification of fulvestrant by GC- or LC-MS. Fulvestrant is a selective estrogen receptor degrader (SERD) that downregulates and degrades estrogen receptor α (ERα). It binds to rat uterine ER with an IC50 value of 44.8 nM and prevents uterine weight increases induced by estradiol in immature rats (ED50 = 0.06 mg/kg per day) but has no effect on uterine weight alone. It also decreases uterine weight in adult rats without affecting the production of luteinizing and follicle-stimulating hormones and prolactin. Fulvestrant inhibits the growth of ER-positive MCF-7 human breast cancer cells but not ER-negative BT-20 cells when used at a concentration of 1 µg/ml. It also prevents tumor growth in MCF-7 and Br10 breast cancer mouse xenograft models when used at a single dose of 5 mg per animal. Fulvestrant is neuroprotective in vitro against neurotoxicity induced by glutamate- and amyloid-β (1-42) (Aβ42) in primary rat hippocampal cells. Formulations containing fulvestrant have been used in the treatment of estrogen-sensitive breast cancer.
| Cas No. | SDF | ||
| 别名 | ICI 182780-d3; ZD 9238-d3; ZM 182780-d3 | ||
| Canonical SMILES | OC1=CC=C2C(C[C@@H](CCCCCCCCCS(CCCC(F)(F)C(F)(F)F)=O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC([2H])([2H])[C@]4([2H])O)=C1 | ||
| 分子式 | C32H44D3F5O3S | 分子量 | 609.8 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 20 mg/ml,Ethanol: 25 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 | 1.6399 mL | 8.1994 mL | 16.3988 mL |
| 5 mM | 0.328 mL | 1.6399 mL | 3.2798 mL |
| 10 mM | 0.164 mL | 0.8199 mL | 1.6399 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。
Liquid chromatography tandem mass spectrometry method for determination of fulvestrant in rat plasma and its application to pharmacokinetic studies of a novel fulvestrant microcrystal
Biomed Chromatogr 2020 Oct;34(10):e4912.PMID:32496589DOI:10.1002/bmc.4912
Fulvestrant ('Faslodex'), an estrogen receptor antagonist, is available for the treatment of advanced breast cancer. The oil-based vehicle of Faslodex can lead to various adverse effects. A novel fulvestrant microcrystal (aqueous suspension) was developed in this study to eliminate these adverse effects. A sensitive and robust liquid chromatography tandem mass spectrometry method was developed and validated for the determination of fulvestrant in rat plasma using supported-liquid extraction. The separation of fulvestrant was achieved on an Agilent SB-C18 column (2.1 × 50 mm, 3.5 μm) with isocratic elution using Fulvestrant-d3 as internal standard. Mass spectrometric detection was conducted in negative multiple reaction monitoring mode. Ion transitions were at m/z 605.5 → 427.5 for fulvestrant and m/z 608.5 → 430.5 for Fulvestrant-d3. The excellent linearity was demonstrated over the range 0.05-100.0 ng/ml (r2 = 0.99). The lower limit of quantitation was 0.05 ng/ml, which was superior to that reported in literature The method validation was evaluated by selectivity, accuracy, precision, recovery and matrix effect in agreement with the US Food and Drug Administration guidance. The method was successfully applied to a pharmacokinetic study of a novel fulvestrant microcrystal in rats after intramuscular administration. It revealed that the rate of absorption increases and the extent of absorption is constant with a decrease in microcrystal diameter.