2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. WRN-IN-24

WRN-IN-24 是一种具有口服活性的变构共价 Werner 综合征 RecQ DNA 解旋酶 (WRN) 抑制剂，其 IC50 为 201 nM。WRN-IN-24 可结合至一个新型变构空腔，与 K894 形成额外氢键，并在功能上抑制 WRN 活性。WRN-IN-24 可抑制结直肠癌细胞增殖，并在异种移植小鼠模型中呈现剂量依赖性抗肿瘤活性。WRN-IN-24 可用于高度微卫星不稳定性癌症的研究，包括结直肠癌。

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

WRN-IN-24

WRN-IN-24 Chemical Structure

CAS No. : 3113010-46-8

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

WRN-IN-24 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

WRN-IN-24 is an orally active allosteric covalent Werner syndrome helicase (WRN) inhibitor with an IC50 of 201 nM. WRN-IN-24 binds to a novel allosteric cavity, forms an additional hydrogen bond with K894, and functionally inhibits WRN activity. WRN-IN-24 inhibits colorectal cancer cells proliferation and exerts dose-dependent antitumor activity in xenograft mouse models. WRN-IN-24 can be used for the research of microsatellite instability-high cancers, including colorectal cancer[1].

体外研究
(In Vitro)

WRN-IN-24 (Compound 22) 可强效抑制纯化的 WRN 解旋酶活性，其 IC50 为 201 nM[1]。
WRN-IN-24 可强效抑制 HCT116 MSI-H 结直肠癌细胞的增殖，其 IC50 为 49 nM[1]。
WRN-IN-24 可在 SW48 MSI-H 结直肠癌细胞中激活 DNA 损伤应答标志物 γH2AX，其 EC50 为 338 nM[1]。
WRN-IN-24 可强效抑制 SW48 MSI-H 结直肠癌细胞的增殖，其 IC50 为 48.0 nM[1]。
WRN-IN-24 对 HT29 和 MDA-MB-231 MSS 细胞系无增殖抑制活性，两者的 IC50 值均 >10000 nM[1]。

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

WRN-IN-24 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route CL Vdss T1/2 Cmax AUC0-last F
Mice[1] 1 mg/kg i.v. 0.82 L/h/kg 3.36 L/kg 3.20 h / / /
Mice[1] 10 mg/kg p.o. / / / 1393 ng/mL 10152 ng·h/mL 98.1 %
Rat[1] 1 mg/kg i.v. 0.70 L/h/kg 2.63 L/kg 4.42 h / / /
Rat[1] 10 mg/kg p.o. / / / 782 ng/mL 7751 ng·h/mL 55.5 %
Dog[1] 1 mg/kg i.v. 0.11 L/h/kg 4.37 L/kg 28.8 h / / /
Dog[1] 5 mg/kg p.o. / / / 869 ng/mL 14960 ng·h/mL 71.5 %
Monkey[1] 1 mg/kg i.v. 0.20 L/h/kg 1.54 L/kg 5.89 h / / /
Monkey[1] 5 mg/kg p.o. / / / 1267 ng/mL 19069 ng·h/mL 82.6 %
体内研究
(In Vivo)

WRN-IN-24 (Compound 22) (5-20 mg/kg；口服；每天一次，21 天) 可在 HCT116 (MSI-H) 异种移植小鼠模型中抑制肿瘤生长[1]。

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

Animal Model: Mice HCT116 (MSI-H) xenograft[1]
Dosage: 5, 10 and 20 mg/kg
Administration: P.o.; daily for 21 days
Result: Inhibited tumor growth with TGI of 95.2% at 20 mg/kg.
Showed ody weight
changes within 15% of the vehicle control group.
分子量

603.63

Formula

C24H28F3N5O6S2
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

WRN-IN-24 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:

WRN-IN-243113010-46-8DNA/RNA SynthesisSW48 MSI-H colorectal cancer cellsK894colorectal cancerHT29 MSS cell linesHCT116 MSI-H colorectal cancer cellsmicrosatellite instability-high cancersMDA-MB-231 MSS cell linesxenograft mouse modelscolorectal cancer cellsWerner syndrome helicaseInhibitorinhibitorinhibit

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：
WRN-IN-24
目录号：
HY-181562
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