2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK11-IN-1 hydrochloride

CDK11-IN-1 hydrochloride 是一种强效、高选择性、口服有效的 CDK11 抑制剂，其 IC50 为 4 nM，对 CDK7、CDK9 的选择性分别 32.5 倍和 2700 倍。CDK11-IN-1 hydrochloride 可竞争性结合CDK11的 ATP 结合口袋，与铰链区残基 Val163 形成氢键。CDK11-IN-1 hydrochloride 可抑制肿瘤细胞增殖，在肺癌异种移植模型中呈现抗肿瘤活性。CDK11-IN-1 hydrochloride 可用于 CDK11 介导的肿瘤病理生理研究，以及肺癌等恶性肿瘤的研究。

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

CDK11-IN-1 hydrochloride

CDK11-IN-1 hydrochloride 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

CDK11-IN-1 hydrochloride 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK11-IN-1 hydrochloride is a potent, highly selective, and orally active CDK11 inhibitor with an IC50 of 4 nM, showing 32.5-fold and 2700-fold selectivity over CDK7 and CDK9, respectively. CDK11-IN-1 hydrochloride binds competitively to the ATP-binding pocket of CDK11 and forms a hydrogen bond with the hinge region residue Val163. It inhibits tumor cell proliferation and exhibits antitumor activity in lung cancer xenograft models. CDK11-IN-1 hydrochloride can be used for studies on the pathophysiology of CDK11-mediated tumors, as well as research on malignant tumors such as lung cancer[1].

IC50 & Target

CDK11

4 nM (IC50)

体外研究
(In Vitro)

CDK11-IN-1 (compound 37) (5 nM-100 μM；72 h) hydrochloride 在 KHOS、LU99 细胞 CellTiter-Glo 活力实验中，对 KHOS 的 GI50 为 3.7 μM、对 LU99 的 GI50 为 0.40 μM[1]。

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

CDK11-IN-1 hydrochloride 相关抗体:

Cell Viability Assay[1]

Cell Line: KHOS, LU99
Concentration: 5 nM, 15 nM, 45 nM, 135 nM, 405 nM, 1.215 μM, 3.645 μM, 10.935 μM, 32.805 μM, 100 μM (3-fold serial dilution)
Incubation Time: 72 h
Result: Inhibited cell proliferation, with GI50 values of 3.7 μM in KHOS cells and 0.40 μM in LU99 cells.
体内研究
(In Vivo)

CDK11-IN-1 (compound 37) (50-200 mg/kg；灌胃；每日 1 次；14 天) hydrochloride 在雌性 BALB/c 裸鼠模型中耐受良好，无明显毒性及体重显著下降[1]。
CDK11-IN-1 (200 mg/kg；灌胃；单次给药；给药后 8 h) hydrochloride 在 LU99 肺癌异种移植 BALB/c 裸鼠模型中，肿瘤内 AUC0-last 为 47074 ng・h/g、Cmax 为 7311 ng/g，肿瘤暴露水平显著高于血浆[1]。
CDK11-IN-1 (10、30、100 mg/kg，100 mg/kg；灌胃；每日 2 次；14 天）hydrochloride 在 LU99 肺癌异种移植 BALB/c 裸鼠模型中，实现 30% 肿瘤生长抑制[1]。

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

Animal Model: Female BALB/c nude mice (7-8 weeks old, unspecified weight) bearing LU99 lung cancer xenografts, anti-tumor efficacy model[1]
Dosage: 10 mg/kg, 30 mg/kg, 100 mg/kg (once daily for 14 days); 100 mg/kg
Administration: 1) once daily for 14 days
2) twice daily for 14 days
Result: Once-daily dosing at 10, 30 or 100 mg/kg did not significantly inhibit tumor growth, while twice-daily dosing at 100 mg/kg produced 30% tumor growth inhibition (TGI); all treatments were well tolerated with no significant body weight loss.
分子量

373.85

Formula

C19H21ClFN5
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

CDK11-IN-1 hydrochloride 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:

CDK11-IN-1CDKCyclin dependent kinaselung cancerCDK7lung tumour modelCDK9CDK11Inhibitorinhibitorinhibit

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：
CDK11-IN-1 hydrochloride
目录号：
HY-182764A
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