2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis Others
  3. PROTACs Estrogen Receptor/ERR Apoptosis Fluorescent Dye
  4. PROTAC ERα Degrader-11

PROTAC ERα Degrader-11 是一种选择性且具有内源荧光 (Ex: 366 nm, Em: 440 nm) 的 ERα PROTAC 降解剂。PROTAC ERα Degrader-11 在 MCF-7 乳腺癌细胞系中展现出良好的抗增殖活性、选择性 ERα 降解能力及荧光成像功能。PROTAC ERα Degrader-11可以诱导 MCF-7 细胞 G2/M 期阻滞和凋亡 (apotosis)。PROTAC ERα Degrader-11 在无胸腺裸鼠中表现出良好的安全性，500 mg/kg 剂量下未见急性毒性反应。PROTAC ERα Degrader-11 可用于乳腺癌相关研究。(粉色：ERα 配体：(HY-167701)，蓝色：CRBN 配体 (HY-150831)，黑色：连接子，E3 连接酶配体-连接子偶联物：HY-174880)。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

PROTAC ERα Degrader-11

PROTAC ERα Degrader-11 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

PROTAC ERα Degrader-11 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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

PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880))[1].

IC50 & Target[1]

ERα

 

ERβ

 

体外研究
(In Vitro)

PROTAC ERα Degrader-11 (Compound W2) (96 h) 表现出优异的细胞抑制活性，其对 MCF-7 细胞的 IC50 值为 0.19 μM，对 MCF-7EGFR 细胞的 IC50 值为 1.40 μM、对 MCF-7D538G 细胞的 IC50 值为 4.31 μM，对 MCF-7Y537S 细胞的 IC50 值为 9.29 μM[1]。

PROTAC ERα Degrader-11 (10 μM, 0-24 h) 在 MCF-7 细胞中以时间依赖性方式降解 ERα，该降解作用在添加 ERα 配体 OBHSA (HY-167701) 或 CRBN 配体后减弱[1]。

PROTAC ERα Degrader-11 (0.5-10 μM, 24 h) 不会降解 PC9 细胞中的ERβ[1]。

PROTAC ERα Degrader-11 (0-80 μM, 10-360 min) 的荧光强度随浓度增加和时间延长呈比例升高[1]。

PROTAC ERα Degrader-11 (1-20 μM, 48 h) 可诱导 MCF-7 细胞发生 G2/M 期阻滞并促进细胞凋亡[1]。

PROTAC ERα Degrader-11 (10 μM, 0-60 min) 在 ERα 存在条件下表现出较高的光稳定性[1]。

PROTAC ERα Degrader-11 (0.1-20 μM) 对 SD 大鼠血细胞膜未造成显著损伤[1]。

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

PROTAC ERα Degrader-11 相关抗体:

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 1, 10 μM
Incubation Time: 48 h
Result: Induced G2/M phase arrest dose-dependently in MCF-7 cells.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 10, 20 μM
Incubation Time: 48 h
Result: Induced apoptosis dose-dependently in MCF-7 cells.
体内研究
(In Vivo)

PROTAC ERα Degrader-11 (Compound W2) (500 mg/kg，单次腹腔注射) 在无胸腺裸鼠中耐受性良好，500 mg/kg 剂量下未表现出急性毒性[1]。

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

Animal Model: Female BALB/C nude mice (5 weeks)[1]
Dosage: 500 mg/kg
Administration: i.p. for single dose
Result: Showed no treatment-related mortality or clinical signs of toxicity (including piloerection, lethargy, or neurological abnormalities).
Showed no abnormality of body weight changed.
分子量

997.00

Formula

C51H47F3N4O12S
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

PROTAC ERα Degrader-11 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

PROTAC ERα Degrader-11PROTAC ERα Degrader11PROTAC ERα Degrader 11PROTACsEstrogen Receptor/ERRApoptosisFluorescent DyeERαMCF-7cancerInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
PROTAC ERα Degrader-11
目录号：
HY-174870
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z