2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. THIQ 40

THIQ-40 是一种基于四氢异喹啉、口服有效和选择性的雌激素受体 ERα 降解剂 (SERD) (IC50=17 nM)，具有抗肿瘤作用。THIQ-40 具有功能性 ERα 拮抗活性，能促进 ERα 降解并形成稳定的 ERαLBD 复合物。THIQ-40 在多物种血浆中表现出快速外消旋化的特征。THIQ-40 可广泛应用于 ERα 阳性乳腺癌的相关机制与药物研发研究。

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

THIQ 40

THIQ 40 Chemical Structure

CAS No. : 1799430-91-3

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

THIQ 40 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

THIQ-40 is a tetrahydroisoquinoline-based, orally active, and selective estrogen receptor ERα degrader (SERD) (IC50=17 nM), with antitumor efficacy. THIQ-40 possesses functional ERα antagonistic activity, promotes ERα degradation and forms stable ERαLBD complexes. THIQ-40 shows the characteristic of rapid racemization in multi-species plasma. THIQ-40 can be widely applied to studies on the relevant mechanisms and drug development of ERα-positive breast cancer[1][2].

IC50 & Target[1]

ERα

 

体外研究
(In Vitro)

THIQ 40 (compound 40) 抑制 MCF-7 人乳腺癌细胞中 ERα 介导的转录，其 IC50 为 30 nM[1]。
THIQ 40 (10 μM; 18-24 h) 可在人乳腺癌 MCF-7 细胞中强效诱导 ERα 降解[1]。
THIQ 40 可抑制胰岛素介导的 MCF-7 人乳腺癌细胞增殖，6 天时的 IC50 为 2.1 nM[1]。

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

THIQ 40 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 10 μM (single dose for % ERα remaining); dose-response series starting at 10 μM (IC50 determination)
Incubation Time: 18-24 h
Result: Reduced ERα protein levels to 15% of control at 10 μM.
Induced ERα degradation with an IC50 of 0.9 nM in initial profiling.
Induced ERα degradation with an IC50 of 1.8 nM in a follow-up assay alongside fulvestrant.
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t CL T1/2 (Elimination) Cmax Tmax Bioavailability
Rat[1] 1 mg/kg i.v. 2627 nM·h/mL 14.9 mL/min/kg 0.8 h / / /
Rat[1] 3 mg/kg p.o. 1586 nM·h/mL / / 1199 nM 0.3 h 60 %
Dog[1] 0.3 mg/kg i.v. 14347 nM·h 2.3 mL/min/kg 5.0 h / / /
Dog[1] 10 mg/kg p.o. 7994 mL/mg/kg / / 1311 nM 1.2 h 56 %
体内研究
(In Vivo)

THIQ 40 (compound 40) (20 mg/kg；口服；每日 1 次) 在补充雌二醇的裸鼠 MCF-7 乳腺癌异种移植模型中，可诱导 78% 的肿瘤生长抑制，并使肿瘤 ERα 水平降低 51%-56%[1]。

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

Animal Model: nude mice (female, immunocompromised)[1]
Dosage: 20 mg/kg
Administration: p.o.; once daily
Result: Induced 78% tumor growth inhibition compared to vehicle control (day 108).
Reduced tumor ERα protein levels by 56% at 7 hours postdose and 51% at 24 hours postdose compared to vehicle control.
Caused no body weight loss in treated mice.
分子量

427.54

Formula

C28H29NO3
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

THIQ 40 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:

THIQ 401799430-91-3THIQ40THIQ-40Estrogen Receptor/ERRMCF-7 breast cancer xenograft modelestrogen receptor degraderMet421ERα+ breast cancerMCF-7 human breast cancer cellsERαHis524nude micehuman ERα LBDSaccharomyces cerevisiae strain LP501Inhibitorinhibitorinhibit

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：
THIQ 40
目录号：
HY-124627
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