Fulvestrant (ICI 182,780). (Synonyms: 氟维司群; ICI 182780; ZD 9238; ZM 182780)
目录号: PC10416 纯度: ≥98%
CAS No. :129453-61-8
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中文名称
Fulvestrant (ICI 182,780).
中文别名
氟维司群;(7a,17b)-7-[9-(4,4,5,5,5-五氟戊亚磺酰基)壬烷基]-雌甾-1,3,5-(10)-三烯-3,17-二醇;氟维斯群;Fulvestrant 抑制剂;比卡鲁胺;氟维司群 EP标准品;氟维司群 USP标准品;氟维司群。;氟维司群-D3;氟维司群标准品;氟维司群系统适用性 EP标准品;氟维司群原药;氟维斯群 API;羟菌唑;氟维司琼;氟维司群杂质;FULVESTRANT氟维司群;7Α-[9-(4,4,5,5,5-五氟戊基亚硫酰基)壬基]雌甾-1,3,5(10)-三烯-3,17Β-二醇;湖北扬信现货供应氟维司群杂质ABCDE
英文名称
Fulvestrant (ICI 182,780)
英文别名
Fulvestrant;(7a,17b)-7-[9-[(4,4,5,5,5-pentafluoropentyl)sulfinyl]nonyl]estra-1,3,5(10)-triene-3,17-diol;Fulvestrant (ICI 182780,ZD 9238, Faslodex®);Fulvestrant Solution;ICI 182,780;(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;Bendamustine hydrochloride;EP3101;Faslodex;SDX105;ZD 182780;ZD9238;ZM182780;Fulvtrant;ICH-182780;Fulvstrant;ICI-187280;Fulvestran;ZD 9238;zd182780
Cas No.
129453-61-8
分子式
C32H47F5O3S
分子量
606.77
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.

性状

Solid

IC50 & Target[1][2]

IC50: 9.4 nM (Estrogen Receptor)

体外研究(In Vitro)

Fulvestrant (ICI 182780; ZD 9238; ZM 182780) is a potent and specific inhibitor of estrogen action and demonstrates excellent growth-inhibitory effects in both cell and animal models of human breast cancer. Fulvestrant inhibits MCF-7 human breast cancer cells growth with the IC50 of 0.29 nM. The relative binding affinities of Fulvestrant is 0.89. Fulvestrant has significantly increased antiestrogenic potency and retains pure estrogen antagonist activity. Fulvestrant is the first of a new type of endocrine treatment-an oestrogen receptor (ER) antagonist that downregulates the ER. Treatment of MCF-7 cells with 1 μM ICI 47699 has no effect on the expression of ERα, whereas 100 nM Fulvestrant completely inhibits ERα expression.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

When administered alone, parenterally (s.c.), to immature female rats Fulvestrant (ICI 182,780) is devoid of uterotropic activity. Complete antagonism of Estrogen action is achieved with a dose of 0.5 mg Fulvestrant/kg/day s.c. The effects of Fulvestrant administered p.o. are qualitatively similar but potency is reduced by an order of magnitude compare with s.c. dosing (ED50 0.46 and complete antagonism at 5 mg/kg/day p.o.). The anti-tumor activity of Fulvestrant is first demonstrated in two models of human breast cancer in nude mice. In one of these models, the growth of MCF-7 tumor xenografts is completely blocked for at least 4 weeks following a single injection of Fulvestrant 5 mg. Similar reductions in growth are seen in the Br10 human tumor model. In other studies in nude mice bearing MCF-7 xenografts, Fulvestrant suppresses the growth of established tumours for twice as long and tumor growth is delayed to a greater extent than is observed with ICI 47699 treatment. ICI 47699-resistant breast tumors, which grow in nude mice after long-term treatment with ICI 47699, remain ensitive to growth inhibition by Fulvestrant. These are comparable to the tumor growth inhibition (TGI) observed for ICI 47699 and Fulvestrant, which on day 40 are 86 and 88%, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial
参考文献
溶解度数据
体外研究: 

DMSO : 250 mg/mL (412.02 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 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 0.8240 mL 1.6481 mL
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产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: 2.75 mg/mL (4.53 mM); Suspended solution; Need ultrasonic

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.12 mM); Suspended solution

    此方案可获得 ≥ 2.5 mg/mL (4.12 mM,饱和度未知) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 15% Solutol HS 15  10% Cremophor EL  35% PEG 400   40% water

    Solubility: 2.5 mg/mL (4.12 mM); Suspended solution; Need ultrasonic

  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (3.43 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (3.43 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 5.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

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搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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