Fulvestrant (ICI 182,780)
(Synonyms: 氟维司群) 目录号 : GC18000
Fulvestrant是一种选择性雌激素受体(ER)拮抗剂。
Cas No.:129453-61-8
Sample solution is provided at 25 µL, 10mM.
Fulvestrant is a selective estrogen receptor (ER) antagonist. It binds, blocks and degrades estrogen receptor, then inhibits estrogen receptor(ER)-mediated transcriptional activity with an IC50 of 9.4 nM [1-3].
Fulvestrant(3 μM ;1 month) increases the sensitivity of H1975 NSCLC cells to gefitinib[4].Fulvestrant(1-10 µM;72 h) strongly sensitized doxorubicin-induced cytotoxicity in MDR cell lines[5].
Fulvestrant(5 mg/mouse; s.c.; twice per week) significantly inhibited macrophage and neutrophil infiltration in mice cancer model. Fulvestrant decreases ER+ breast cancer growth in the presence of physiologic levels of estradiol in human breast cancer in nude mice[6]. Fulvestrant (5mg/mouse; twice weekly; s.c.) in combination with tamoxifen enhanced tumor regression[7].
References:
[1]. Vergote I, Robertson JF. Fulvestrant is an effective and well-tolerated endocrine therapy for postmenopausal women with advanced breast cancer: results from clinical trials. Br J Cancer. 2004 Mar;90 Suppl 1(Suppl 1):S11-4. doi: 10.1038/sj.bjc.6601631. PMID: 15094759; PMCID: PMC2750769.
[2]. Osborne CK, Wakeling A, et,al. Fulvestrant: an oestrogen receptor antagonist with a novel mechanism of action. Br J Cancer. 2004 Mar;90 Suppl 1(Suppl 1):S2-6. doi: 10.1038/sj.bjc.6601629. PMID: 15094757; PMCID: PMC2750773.
[3]. Dowsett M, Nicholson RI, et,al. Biological characteristics of the pure antiestrogen fulvestrant: overcoming endocrine resistance. Breast Cancer Res Treat. 2005;93 Suppl 1:S11-8. doi: 10.1007/s10549-005-9037-3. PMID: 16247595.
[4]. Shen H, Liu J, et,al. Fulvestrant increases gefitinib sensitivity in non-small cell lung cancer cells by upregulating let-7c expression. Biomed Pharmacother. 2014 Apr;68(3):307-13. doi: 10.1016/j.biopha.2013.10.007. Epub 2013 Nov 7. PMID: 24268810.
[5]. Huang Y, Jiang D, et,al. Fulvestrant reverses doxorubicin resistance in multidrug-resistant breast cell lines independent of estrogen receptor expression. Oncol Rep. 2017 Feb;37(2):705-712. doi: 10.3892/or.2016.5315. Epub 2016 Dec 14. PMID: 28000875; PMCID: PMC5355712.
[6]. Abrahamsson A, Rodriguez GV, et,al. Fulvestrant-Mediated Attenuation of the Innate Immune Response Decreases ER+ Breast Cancer Growth In Vivo More Effectively than Tamoxifen. Cancer Res. 2020 Oct 15;80(20):4487-4499. doi: 10.1158/0008-5472.CAN-20-1705. Epub 2020 Aug 27. PMID: 32855207.
[7]. Mishra AK, Abrahamsson A, et,al. Fulvestrant inhibits growth of triple negative breast cancer and synergizes with tamoxifen in ERα positive breast cancer by up-regulation of ERβ. Oncotarget. 2016 Aug 30;7(35):56876-56888. doi: 10.18632/oncotarget.10871. PMID: 27486755; PMCID: PMC5302959.
Fulvestrant是一种选择性雌激素受体(ER)拮抗剂。它结合、阻断和降解estrogen receptor(ER)，然后抑制estrogen receptor(ER)介导的转录活性，IC50为9.4 nM[1-3]。
Fulvestrant (3 μM ;1 month)增加H1975 NSCLC细胞对吉非替尼的敏感性[4]。Fulvestrant (1-10 µM;72 h)对多耐药细胞系中阿霉素诱导的细胞毒性具有强致敏作用[5]。Fulvestrant (5 mg/mouse; s.c.; twice per week) 显著抑制小鼠肿瘤模型中巨噬细胞和中性粒细胞的浸润。在裸鼠人乳腺癌中，在存在生理水平雌二醇的情况下，Fulvestrant可降低ER+乳腺癌的生长[6]。Fulvestrant (5mg/mouse; twice weekly; s.c.)联合tamoxifen可促进肿瘤消退[7]。
|
Cell experiment [1]: |
|
|
Cell lines |
Bats-72 cell line (estrogen receptor-negative MDR cell line) |
|
Preparation method |
Cells were exposed to designated concentrations of doxorubicin with or without co-treatment of fulvestrant for 72 h, the cell viabilities were determined. |
|
Reaction Conditions |
1-10 µM;72 h |
|
Applications |
Fulvestrant sensitizes doxorubicin-induced cytotoxicity in estrogen receptor-negative MDR cell line Bats-72. |
|
Animal experiment [2]: |
|
|
Animal models |
Balb/C-nu/nu mice (MCF7 cells model) |
|
Preparation method |
Mice were treated with fulvestrant in addition to the estradiol exposure. |
|
Dosage form |
5 mg/mouse; s.c.; twice per week |
|
Applications |
Fulvestrant significantly inhibited macrophage and neutrophil infiltration in mice cancer model. |
|
References: [1]. Huang Y, Jiang D,et,al. Fulvestrant reverses doxorubicin resistance in multidrug-resistant breast cell lines independent of estrogen receptor expression. Oncol Rep. 2017 Feb;37(2):705-712. doi: 10.3892/or.2016.5315. Epub 2016 Dec 14. PMID: 28000875; PMCID: PMC5355712. [2]. Abrahamsson A, Rodriguez GV, et,al. Fulvestrant-Mediated Attenuation of the Innate Immune Response Decreases ER+ Breast Cancer Growth In Vivo More Effectively than Tamoxifen. Cancer Res. 2020 Oct 15;80(20):4487-4499. doi: 10.1158/0008-5472.CAN-20-1705. Epub 2020 Aug 27. PMID: 32855207. |
|
| Cas No. | 129453-61-8 | SDF | |
| 别名 | 氟维司群 | ||
| 化学名 | (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol | ||
| Canonical SMILES | CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F | ||
| 分子式 | C32H47F5O3S | 分子量 | 606.77 |
| 溶解度 | ≥ 30.35mg/mL 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6481 mL | 8.2404 mL | 16.4807 mL |
| 5 mM | 0.3296 mL | 1.6481 mL | 3.2961 mL |
| 10 mM | 0.1648 mL | 0.824 mL | 1.6481 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
-
Related Biological Data
The change fold of (A) T, (B) 11-KT, (C) 17β-E2, (D) VTG in plasma of male and female zebrafish in dienestrol (ER agonist), fulvestral (ER antagonist),dihydrotestosterone (AR agonist), flutamide (AR antagonist) and different EHDPHP treatment groups (2.5, 50, 250 μg/L) compared with the control group (treated with 0.01% DMSO) and the values are expressed as mean ± standard error.
The concentration of DHT,DIES, FLU and FUL (Glpbio)was set at 10 nM.
Environment International 158 (2022): 106928. PMID: 34638023 IF: 9.623 -
Related Biological Data
E2 decreases neutrophils in c-mybhyper transgenic zebrafish embryos through ERs-independent mechanisms. G ICI 182780 did not alleviate E2-mediated inhibition of c-mybhyper zebrafish neutrophils.
The following compounds were used:DMSO; 17β-estradiol; 2,3-bis(4-hydroxyphenyl) propionitrile (DPN:50 μM, glpbio, GC17688); propyl pyrazole triol (PPT: 50 μM, glpbio, GC14370); fulvestrant (ICI-182,780:15 μM, glpbio, GC18000), G1 , E2 ELISA kit and PX-478 or compounds from the compound library.
Cell Death Discovery 8.1 (2022): 1-12. PMID: 35842445 IF: 7.1089 -
Related Biological Data
The e ects of ICI182780 treatment on the mRNA expression of Akt and β-catenin.
For ERα blocking test, the culture system on day 7 was treated with either placebo or 200 nM ICI182780 (GlpBio, co., Ltd., Montclair, NJ, USA) to block ERα pathways.
Int J Env Res Pub He 16.19 (2019): 3779. PMID: 31597358 IF: 2.007