2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Brilanestrant

Brilanestrant  (Synonyms: ARN-810; GDC-0810)

目录号: HY-12864 纯度: 99.95%
COA 产品使用指南

摩尔计算器

Brilanestrant (ARN-810; GDC-0810) 是一种可口服的，选择性的雌激素降能器 (selective estrogen receptor degrader)，IC50 值为 0.7 nM。

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Brilanestrant Chemical Structure

Brilanestrant Chemical Structure

CAS No. : 1365888-06-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1045
In-stock
2 mg ￥480
In-stock
5 mg ￥950
In-stock
10 mg ￥1425
In-stock
25 mg ￥2600
In-stock
50 mg ￥3770
In-stock
100 mg ￥5500
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Brilanestrant 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Brilanestrant (ARN-810; GDC-0810) is an orally bioavailable selective estrogen receptor degrader (SERD) with IC50 of 0.7 nM.

IC50 & Target

IC50: 0.7 nM (estrogen receptor)
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 EC50
0.0007 μM
Compound: 11l, GDC-0810, ARN-810
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
[PMID: 25879485]
MCF7 IC50
0.002 μM
Compound: 11l, GDC-0810, ARN-810
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
[PMID: 25879485]
MCF7 EC50
0.7 nM
Compound: ARN-810; 3
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal-stripped FBS incubated for 4 hrs by IRDye 800CW/DRAQ5 dye based in-cell Western assay
[PMID: 30587451]
MCF7 EC50
0.7 nM
Compound: 2; ARN-810
Decrease in estrogen receptor alpha level in human MCF7 cells after 4 hrs by in-cell western assay
Decrease in estrogen receptor alpha level in human MCF7 cells after 4 hrs by in-cell western assay
[PMID: 26463130]
MCF7 IC50
0.85 nM
Compound: 2; GDC-0810
Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis
Induction of ERalpha degradation in human MCF7 cells after 4 hrs by FITC/Hoechst staining based immunofluorescence imaging analysis
[PMID: 32551022]
MCF7 EC50
17 nM
Compound: 10; GDC-0810
Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay
Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay
[PMID: 34251202]
MCF7 IC50
2 nM
Compound: 11l, GDC-0810, ARN-810
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
[PMID: 25879485]
MCF7 IC50
2.5 nM
Compound: 2; ARN-810
Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 5 days by celltiterGlo assay
Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 5 days by celltiterGlo assay
[PMID: 26463130]
MCF7 IC50
2.5 nM
Compound: ARN-810; 3
Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell proliferation measured after 5 days by Cell-titer-Glo assay
[PMID: 30587451]
MCF7 IC50
44 nM
Compound: 2; GDC-0810
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by Celltiter-Glo assay
[PMID: 32551022]
体外研究
(In Vitro)

Brilanestrant (ARN-810; GDC-0810) is a potent ER-α binder (IC50=6.1 nM), a full transcriptional antagonist with no agonism (3× ERE, IC50=2 nM), and displays good potency and efficacy in ER-α degradation (EC50=0.7 nM) and MCF-7 breast cancer cell viability (IC50=2.5 nM) assays[1].Brilanestrant (ARN-810; GDC-0810) induces a distinct ERα conformation versus tamoxifen and other ER therapeutics, and does not exhibit tamoxifen-like ER agonism in MCF7 cells[2].

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

Brilanestrant 相关抗体:
体内研究
(In Vivo)

The pharmacokinetic profile of Brilanestrant (ARN-810) shows it is a olw clearance molecule across species, with good bioavailability (40%-60%). Brilanestrant (ARN-810) (3 mg/kg, p.o.) shows substantial tumor-growth inhibition in a tamoxifen-sensitive MCF-7 xenograft model, while at the highest dose of 100 mg/kg/day, all animals show tumor regression of more than 50% without weight loss[1].
Brilanestrant (ARN-810) exhibits low clearance (11 mL/min/kg) and 61% oral bioavailability. Brilanestrant (ARN-810) (1-100 mg/kg/day, p.o.) displays dose dependent efficacy in the MCF7 xenograft model[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

446.90

Formula

C26H20ClFN2O2
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (223.76 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2376 mL 11.1882 mL 22.3764 mL
5 mM 0.4475 mL 2.2376 mL 4.4753 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.59 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.59 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    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玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.95%

COA (292 KB) LCMS (259 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[1]

MCF-7 cells are adjusted to a concentration of 40000 cells per mL in RPMI containing 10% FBS and 20 mM HEPES. Then 16 μL of the cell suspension (640 cells) is added to each well of a 384-well plate, and the cells are incubated overnight to allow the cells to adhere. The following day a 10-point, serial 1:5 dilution of each compound is added to the cells in 16 μL at a final concentration ranging from 10 to 0.000005 μM. After 5 days' compound exposure, 16 μL of CellTiter-GLo is added to the cells, and the relative luminescence units of each well are determined. CellTiter-GLo added to 32 μL of medium without cells is used to obtain a background value. The percent viability of each sample is determined as follows: (RLU sample-RLU background/RLU untreated cells-RLU background ×100=%viability)

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Time release pellets containing 0.72 mg 17-β estradiol are subcutaneously implanted into nu/nu mice. MCF-7 cells are grown in RPMI containing 10% FBS at 5% CO2 37°C. Trypsinized cells are pelleted and resuspended in 50% RPMI（serum free）and 50% Matrigel at 1×107 cells/mL. MCF-7 cells are subcutaneously injected (100 μL/animal) on the right flank 2-3 days post pellet implantation. Tumor volume (length × width2/2) is monitored biweekly. When tumors reach an average volume of appr 200 mm3 animals are randomized and treatment is started. Animals are treated with vehicle or compound daily for 4 weeks. Tumor volume and body weight are monitored biweekly throughout the study.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Brilanestrant 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2376 mL 11.1882 mL 22.3764 mL 55.9409 mL
5 mM 0.4475 mL 2.2376 mL 4.4753 mL 11.1882 mL
10 mM 0.2238 mL 1.1188 mL 2.2376 mL 5.5941 mL
15 mM 0.1492 mL 0.7459 mL 1.4918 mL 3.7294 mL
20 mM 0.1119 mL 0.5594 mL 1.1188 mL 2.7970 mL
25 mM 0.0895 mL 0.4475 mL 0.8951 mL 2.2376 mL
30 mM 0.0746 mL 0.3729 mL 0.7459 mL 1.8647 mL
40 mM 0.0559 mL 0.2797 mL 0.5594 mL 1.3985 mL
50 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
60 mM 0.0373 mL 0.1865 mL 0.3729 mL 0.9323 mL
80 mM 0.0280 mL 0.1399 mL 0.2797 mL 0.6993 mL
100 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5594 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Brilanestrant1365888-06-7ARN-810 GDC-0810ARN810ARN 810GDC0810GDC 0810GDC-0810Estrogen Receptor/ERRInhibitorinhibitorinhibit

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