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Fulvestrant (ICI 182,780)

现货
Catalog No.
A1428
雌激素受体拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
25mg
¥ 500.00
现货
100mg
¥ 1,000.00
现货

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Background

Fulvestran is a newer type of estrogen receptor (ER) antagonist with IC50 value of 9.4nM [1].

Fulvestrant treatment caused a significant decrease in MDM2 protein expression in human breast cancer cell lines MCF7 and T47D, and that the reduction of MDM2 correlated with the decrease in ER expression [1].

Fulvestrant enhances the sensitivity of human breast cancer cells to chemotherapeutic drugs. CompuSyn analyses showed that combined use of doxorubicin, paclitaxel or etoposide with fulvestrant resulted in different degrees of synergism in MCF7 and T47D cell lines tested. Besides, Combination of fulvestrant and chemotherapeutic drugs induces altered cell cycle distribution, apoptosis, and senescence [1].

References:
[1] Dolfi SC1, Jäger AV2, Medina DJ1, Haffty BG3, Yang JM4, Hirshfield KM5.Fulvestrant treatment alters MDM2 protein turnover and sensitivity of human breast carcinoma cells to chemotherapeutic drugs. Cancer Lett. 2014 Apr 18. pii: S0304-3835(14)00215-8.

 

文献引用

1. Bai Y, Shen W, et al. "Combined detection of estrogen and tumor markers is an important reference factor in the diagnosis and prognosis of lung cancer." J Cell Biochem. 2018 Sep 14. PMID:30216488
2. McDermott MS, Chumanevich AA, et al. "Inhibition of CDK8 mediator kinase suppresses estrogen dependent transcription and the growth of estrogen receptor positive breast cancer." Oncotarget. 2017 Feb 21;8(8):12558-12575. PMID:28147342
3. Li, Han, et al. "Triptolide inhibits human breast cancer MCF-7 cell growth via downregulation of the ERα-mediated signaling pathway." Acta Pharmacologica Sinica (2015). PMID:25864647

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt606.77
Cas No.129453-61-8
FormulaC32H47F5O3S
Solubility≥30.35mg/mL in DMSO
Chemical Name(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
SDFDownload SDF
Canonical SMILESCC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

T47D和MCF7乳腺癌细胞系

溶解方法

该化合物在DMSO中的溶解度大于30.3 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

1 μM,10 μM,66 h

应用

在ER+人乳腺癌细胞系MCF7和T47D细胞中,fulvestrant治疗显著降低MDM2蛋白表达。Fulvestrant治疗16小时或66小时对MDM2 mRNA水平没有影响。Fulvestrant(1 μM,16h)促进MDM2蛋白的降解并缩短该蛋白的半衰期,在T47D细胞中由42分钟变为27分钟,而MCF7细胞中由180分钟缩短为80分钟。Fulvestrant(5 μM,72h)增加了G1期细胞数目。

动物实验 [2]:

动物模型

携带MCF-7和Br10人乳腺癌的裸鼠

给药剂量

皮下注射,5 mg,4周

应用

Fulvestrant 减少肿瘤生长。

临床试验[3]:

临床试验

晚期乳腺癌的绝经后妇女

剂量

肌内注射,250 mg,每月一次

应用

针对已经进行内分泌治疗的患有晚期乳腺癌的绝经后妇女,Fulvestrant具有有效性和良好的耐受性。

其他注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Dolfi SC1, Jger AV2, Medina DJ1, Haffty BG3, Yang JM4, Hirshfield KM5.Fulvestrant treatment alters MDM2 protein turnover and sensitivity of human breast carcinoma cells to chemotherapeutic drugs. Cancer Lett. 2014 Apr 18. pii: S0304-3835(14)00215-8.

[2]. Wakeling A E, Dukes M, Bowler J. A potent specific pure antiestrogen with clinical potential[J]. Cancer research, 1991, 51(15): 3867-3873.

[3]. Howell A, Robertson J F R, Quaresma Albano J, et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment[J]. Journal of Clinical Oncology, 2002, 20(16): 3396-3403.

质量控制

化学结构

Fulvestrant

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Fulvestrant (ICI 182,780)

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