2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. GNE-149

GNE-149 是一种有效的，具有口服活性的雌激素受体 α (ERα; IC50=0.053 nM) 拮抗剂。GNE-149 也是一种选择性的雌激素受体降解剂 (SERD)。GNE-149 可用于乳腺癌的研究。

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GNE-149 Chemical Structure

GNE-149 Chemical Structure

CAS No. : 1953132-75-6

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Customer Review

GNE-149 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

查看所有亚型
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer[1].

IC50 & Target[1]

ERα

0.053 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 IC50
0.053 nM
Compound: 12; GNE-149
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 IC50
0.66 nM
Compound: 12; GNE-149
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]
MCF7 IC50
0.66 nM
Compound: 1 (GNE-149)
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured by CellTiter-Glo luminescent assay assay
Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability measured by CellTiter-Glo luminescent assay assay
[PMID: 34425201]
MCF7 EC50
0.7 nM
Compound: 13; GNE-149
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]
体外研究
(In Vitro)

GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC50s of 0.66 and 0.69 nM, respectively[1].
GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC50s of 0.053 and 0.031 nM, respectively[1].

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

GNE-149 相关抗体:
体内研究
(In Vivo)

GNE-149 (0.3-30 mg/kg) exhibits in vivo efficacy in an MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant[1].
GNE-149 has favorable pharmacokinetic profile, including total clearance (CL; 19, 8, and 13 mL/min/kg for Rat, Dog, and Cyno) and oral bioavailability (F; 31%, 49%, and 28% for Rat, Dog, and Cyno)[1].

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

Animal Model: Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor[1]
Dosage: 0.3, 1, 3, 10, and 30 mg/kg
Administration: Orally q.d. for 21 days
Result: Exhibited dose-dependent efficacy in the MCF7 WT and Y537S mutant xenograft model, with tumor regression observed at all doses above 0.3 mg/kg in Y537S mutant xenograft model.
分子量

503.57

Formula

C28H33F4N3O
CAS 号
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (99.29 mM; 超声助溶 (<60°C); 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 1.9858 mL 9.9291 mL 19.8582 mL
5 mM 0.3972 mL 1.9858 mL 3.9716 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, 6 months; -20°C, 1 month (protect from light)。-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。

  • 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
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

GNE-149 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, 6 months; -20°C, 1 month (protect from light)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9858 mL 9.9291 mL 19.8582 mL 49.6455 mL
5 mM 0.3972 mL 1.9858 mL 3.9716 mL 9.9291 mL
10 mM 0.1986 mL 0.9929 mL 1.9858 mL 4.9646 mL
15 mM 0.1324 mL 0.6619 mL 1.3239 mL 3.3097 mL
20 mM 0.0993 mL 0.4965 mL 0.9929 mL 2.4823 mL
25 mM 0.0794 mL 0.3972 mL 0.7943 mL 1.9858 mL
30 mM 0.0662 mL 0.3310 mL 0.6619 mL 1.6549 mL
40 mM 0.0496 mL 0.2482 mL 0.4965 mL 1.2411 mL
50 mM 0.0397 mL 0.1986 mL 0.3972 mL 0.9929 mL
60 mM 0.0331 mL 0.1655 mL 0.3310 mL 0.8274 mL
80 mM 0.0248 mL 0.1241 mL 0.2482 mL 0.6206 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:

GNE-1491953132-75-6GNE149GNE 149Estrogen Receptor/ERRMCF7T47DERαSERDantagonistbreast cancerpure antiestrogenestrogen receptorERα antagonistselective estrogen receptor degraderInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-145341
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