2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Estrogen Receptor/ERR Caspase Bcl-2 Family
  4. Estrogen receptor modulator 10

Estrogen receptor modulator 10 

目录号: HY-155406
产品使用指南

摩尔计算器

Estrogen receptor modulator 10 (compound G-5b) 是雌激素受体 (ER) 拮抗剂 (IC50=6.7 nM) 和降解剂 (DC50=0.4 nM)。Estrogen receptor modulator 10 是基于 Fulvestrant (HY-13636) 分子开发的，可以通过蛋白酶体途径迅速降解 ER 受体。Estrogen receptor modulator 10 可以诱导细胞凋亡，把细胞阻滞在G1/G0 期。Estrogen receptor modulator 10 能够用于癌症的研究。

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Estrogen receptor modulator 10 Chemical Structure

Estrogen receptor modulator 10 Chemical Structure

CAS No. : 2991504-90-4

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Estrogen receptor modulator 10 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

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research[1].

IC50 & Target

IC50=6.7 nM, DC50=0.4 nM
体外研究
(In Vitro)

Estrogen receptormodulator 10 (20-100 nM, 2-48 h) 在 T47D 细胞中以剂量依赖性的方式显著降低 ER 的活性，在MCF-7 细胞中对细胞 ER 的降解水平比在 T47D 细胞中晚[1]。
Estrogen receptormodulator 10 (10 nM, 24 h) 在 MCF-7 和T47D 细胞中能够降低 E2 刺激产生的TFF-1 (trefoil factor 1)、 PgR (progesterone receptor) and GRBE1 (growth regulation by estrogen in breast cancer 1) 的表达[1]。
Estrogen receptormodulator 10 (4-100 nM, 24 h) 在 MCF-7 细胞中能够诱导细胞凋亡，显著增强了 caspase-3 和 caspase-9 的活性[1]。
Estrogen receptormodulator 10 (4-100 nM, 24 h) 在 MCF-7 细胞中能够抑制G1/G0 期蛋白的表达[1]。
Estrogen receptormodulator 10 (0.2-1 nM, 6 d) 显著抑制了由 E2 介导的 MCF-7 和 T47D 细胞的增殖[1]。
Estrogen receptormodulator 10 (4-100 nM, 24 h) 在 MCF-7 细胞中显著降低了细胞迁移和增殖细胞核抗原水平[1]。
Estrogen receptormodulator 10 (20-100 nM, 24 h) 在 MCF-7 细胞中降低了细胞质和细胞核中的 ER，促进 ER 从细胞核转到细胞质中。ER通过蛋白酶体途径迅速降解，而不影响相应mRNA的表达[1]。

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

Estrogen receptor modulator 10 相关抗体:

Cell Viability Assay[1]

Cell Line: T47D, MCF-7
Concentration: 100 nM
Incubation Time: 24 h
Result: Significantly decreased the activity of ER in a dose-dependent manner.

RT-PCR[1]

Cell Line: T47D, MCF-7
Concentration: 10 nM
Incubation Time: 24 h
Result: Had antagonistic activity against ER signaling.

Cell Cycle Analysis[1]

Cell Line: MCF-7
Concentration: 4 nM, 20 nM, 100 nM
Incubation Time: 24 h
Result: Blocked cells in the G1/G0 phase with a dose-dependent manner.

Cell Proliferation Assay[1]

Cell Line: T47D, MCF-7
Concentration: 0.2 nM for MCF-7 cells
1 nM for T47D cells
Incubation Time: 6 d
Result: Could selectively inhibit the proliferation and migration of ER-positive breast cancer cells without affecting ER-negative ones.

Cell Proliferation Assay[1]

Cell Line: T74DWT, T74DY537S, T74DD538G
Concentration: 2.21 nM for T74DWT
5.94 nM for T74DY537S
58.57 nM for T74DD538G
Incubation Time: 5 d
Result: Inhibited mutant cell proliferation in a dose-dependent manner.
体内研究
(In Vivo)

Estrogen receptormodulator 10 (30 mg/kg, 肌肉注射 (i.m.), 单剂量) 在雌性 Sprague-Dawley小鼠中有良好的药代动力学特性[1]。

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

Animal Model: Female Sprague-Dawley Rats[1]
Dosage: 30 mg/kg
Administration: Intramuscular injection (i.m.), single dose
Result: Showed apparent distribution volume (Vz_F_obs≈1600 L) was nearly 1.3 times smaller than that of fulvestrant (Vz_F_obs≈2100 L), and most drugs could be widely distributed from blood to target tissues and organs.
分子量

728.71

Formula

C32H37F9N4O3S
CAS 号
运输条件

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

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Estrogen receptor modulator 10 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

Estrogen receptor modulator 102991504-90-4Estrogen receptor modulator10Estrogen receptor modulator-10Estrogen Receptor/ERRCaspaseBcl-2 FamilyTumorAntagonistDegraderPharmacokineticsPharmacodynamics propertiesMCF-7T47DFemale Sprague-Dawley RatsBreast cancerInhibitorinhibitorinhibit

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