Erteberel

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Erteberel

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

533884-09-2

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
1mg	电议
5mg	电议
10mg	电议
50mg	电议

产品名称

LY500307

产品介绍

Erteberel (LY500307) 是有效，选择性的雌激素受体 β (ERβ) 激动剂，K_i和EC₅₀分别为1.54 nM，3.61 nM。抗肿瘤活性。

生物活性

Erteberel (LY500307) is a potent and selectiveestrogen receptorbeta (ERβ) agonist withK_iandEC₅₀of 1.54 nM and 3.61 nM, respectively^[1]. Anti-tumor activities^[2].

IC₅₀& Target

ERβ

1.54 nM (Ki)

ERβ

3.61 nM (EC₅₀)

体外研究
(In Vitro)

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

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].

体内研究
(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].

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

性状

Solid

Formula

C₁₈H₁₈O₃

CAS 号

533884-09-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 30 mg/mL(106.26 mM)

*"≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量

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
10 mM	0.3542 mL	1.7710 mL	3.5420 mL

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。