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  1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. Erteberel

Erteberel (LY500307) 是有效,選擇性的雌激素受體 β (ERβ) 激動劑,KiEC50 分別為1.54 nM,3.61 nM。Erteberel 與抗腫瘤活性。

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Erteberel Chemical Structure

Erteberel Chemical Structure

CAS No. : 533884-09-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ¥5901
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1 mg ¥1900
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5 mg ¥5500
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Other Forms of Erteberel:

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻

查看 Estrogen Receptor/ERR 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Erteberel (LY500307) is a potent and selective estrogen receptor beta (ERβ) agonist with Ki and EC50 of 1.54 nM and 3.61 nM, respectively. Erteberel has anti-tumor activities[1][2].

IC50 & Target

ERβ

1.54 nM (Ki)

ERβ

3.61 nM (EC50)

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
PC-3 EC50
0.66 nM
Compound: 7a, SERBA-1
Activity at ERbeta in PC3 cells by transcription assay
Activity at ERbeta in PC3 cells by transcription assay
[PMID: 17034120]
PC-3 EC50
19.4 nM
Compound: 7a, SERBA-1
Activity at ERalpha in PC3 cells by transcription assay
Activity at ERalpha in PC3 cells by transcription assay
[PMID: 17034120]
體外研究
(In Vitro)

Treatment with Erteberel (0.25-10 μM, 72 hours) significantly reduces the proliferation of GBM cells with no activity on normal astrocytes in vitro[2].

Erteberel promotes apoptosis of GBM cells. Erteberel modulated several pathways related to apoptosis, cell cycle, and DNA damage response[2].

Erteberel (0-1000 μM) sensitizes GBM cells to several FDA-approved chemotherapeutic drugs including cisplatin, lomustine and temozolomide[2].

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

Cell Viability Assay[2]

Cell Line: U87, U251,T98G and normal astrocytes
Concentration: 0.25, 0.5, 1, 2, 4, 6, 8, and 10 μM
Incubation Time: 72 h
Result: Treatment with Erteberel significantly reduces the viability of various GBM cell lines in a dose-dependent manner. In contrast, viability of normal astrocytes is not affected at the tested doses, suggesting that Erteberel has tumor cell–specific activity[2].
體內(nèi)研究
(In Vivo)

Erteberel (5?mg/Kg body weight/day, oral, 28 days) treatment significantly reduces tumor growth and promotes apoptosis of GBM tumors in an orthotopic model[2].

Erteberel (5?mg/Kg body weight/day, oral, 40-50 days) treatment improves the overall survival of tumor-bearing mice in the GL26 syngeneic glioma model[2].

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

Animal Model: Athymic mice (5-7 weeks) inoculated with OVCAR-3 cells[2]
Dosage: 5mg/Kg body weight
Administration: Oral, daily for 28 days
Result: Immunohistochemical analysis reveals that Erteberel treatment significantly reduces the number of proliferation marker Ki-67-positive cells and increases the number of TUNEL-positive apoptotic cells[2].
Clinical Trial
分子量

282.33

Formula

C18H18O3

CAS 號
性狀

固體

顏色

Off-white to light brown

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : ≥ 30 mg/mL (106.26 mM; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.5420 mL 17.7098 mL 35.4195 mL
5 mM 0.7084 mL 3.5420 mL 7.0839 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.87%

參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.5420 mL 17.7098 mL 35.4195 mL 88.5489 mL
5 mM 0.7084 mL 3.5420 mL 7.0839 mL 17.7098 mL
10 mM 0.3542 mL 1.7710 mL 3.5420 mL 8.8549 mL
15 mM 0.2361 mL 1.1807 mL 2.3613 mL 5.9033 mL
20 mM 0.1771 mL 0.8855 mL 1.7710 mL 4.4274 mL
25 mM 0.1417 mL 0.7084 mL 1.4168 mL 3.5420 mL
30 mM 0.1181 mL 0.5903 mL 1.1807 mL 2.9516 mL
40 mM 0.0885 mL 0.4427 mL 0.8855 mL 2.2137 mL
50 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7710 mL
60 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
80 mM 0.0443 mL 0.2214 mL 0.4427 mL 1.1069 mL
100 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 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.

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產(chǎn)品名稱:
Erteberel
目錄號:
HY-18295
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