2. Cell Cycle/DNA Damage Apoptosis
  3. CDK Apoptosis
  4. CDK9-IN-40

CDK9-IN-40 是一种口服有效的 CDK9 抑制剂，其 IC50 为 5.5 nM。CDK9-IN-40 对 CDK1、CDK2、CDK4和CDK6 的活性较弱。CDK9-IN-40 可阻滞细胞周期、诱导细胞凋亡 (apoptosis ) 并抑制肿瘤生长。CDK9-IN-40 具有很强的抗癌活性。

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

CDK9-IN-40 Chemical Structure

CDK9-IN-40 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

CDK9-IN-40 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK9-IN-40 is a potent and orally active CDK9 inhibitor with an IC50 of 5.5 nM. CDK9-IN-40 shows high selectivity for CDK9 versus CDK1, CDK2, CDK4, and CDK6, respectively. CDK9-IN-40 can arrest cell cycle, induce cell apoptosis and inhibit tumor growth. CDK9-IN-40 exhibits strong anti-cancer activity[1].

体外研究
(In Vitro)

CDK9-IN-40 (Compound 8e) (1.0 μM, 48 h) 对 CDK9 表现出最高的抑制活性 (99% 抑制, IC50 = 5.5 nM)，并且对 CDK9 的选择性分别是 CDK1 和 CDK2的 180 和 75 倍以上[1]。
CDK9-IN-40 (1.8 μM-3.0 μM, 48 h) 对 HeLa、A549、HCT116 和 MCF-7 细胞具有显著的细胞生长抑制活性，其活性大于或接近 ZK 304709[1]。
CDK9-IN-40 (1 μM-4 μM, 24 h) 可使 HCT116 细胞阻滞于 G2/M 期，并诱导细胞凋亡，且呈浓度依赖性[1]。

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

CDK9-IN-40 相关抗体:

Cell Proliferation Assay[1]

Cell Line: HeLa, A549, HCT116, MCF-7, HEK293, LO2
Concentration: 1 μM
Incubation Time: 48 h
Result: Offered the best CDK9 inhibitory activities (IC50 = 5.5 nM), being comparable to that of ZK304709 (IC50 = 5.0 nM) and higher than AZD5438 (IC50 = 18.0 nM).
Didn’t demonstrate obvious cytotoxic activity against two non-tumoural cells HEK-293 and LO2 (IC50 50 μM).

Cell Cycle Analysis[1]

Cell Line: HCT116
Concentration: 1.0 μM, 2.0 μM, 4.0 μM
Incubation Time: 24 h
Result: Induced a dose-dependent G2/M phase arrest (14.71%, 18.16%, and 24.81% respectively).

Apoptosis Analysis[1]

Cell Line: HCT116
Concentration: 1.0 μM, 2.0 μM, 4.0 μM
Incubation Time: 24 h
Result: Induced total apoptosis rates of 10.08%, 16.43%, and 33.70% with the rate of 1.0, 2.0 and 4.0 μM, respectively.
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. T1/2 6.5 hr
Rat 10 mg/kg p.o. T1/2 3.6 hr
Rat 1 mg/kg i.v. Tmax 0.083 hr
Rat 10 mg/kg p.o. Tmax 4.0 hr
Rat 1 mg/kg i.v. MRT0-t 5.4 hr
Rat 10 mg/kg p.o. MRT0-t 125.2 hr
Rat 1 mg/kg i.v. MRT0-∞ 8.4 hr
Rat 10 mg/kg p.o. MRT0-∞ 155.8 hr
Rat 1 mg/kg i.v. AUC0-t 26.5 ng·h/mL
Rat 10 mg/kg p.o. AUC0-t 6.9 ng·h/mL
Rat 1 mg/kg i.v. AUC0-∞ 33.1 ng·h/mL
Rat 10 mg/kg p.o. AUC0-∞ 7.9 ng·h/mL
Rat 1 mg/kg i.v. CL 51.9 L/h/kg
Rat 10 mg/kg p.o. CL 117.2 L/h/kg
Rat 1 mg/kg i.v. Vz 375.3 L/kg
Rat 10 mg/kg p.o. Vz 628.7 L/kg
Rat 1 mg/kg i.v. Cmax 15.9 ng/mL
Rat 10 mg/kg p.o. Cmax 18.6 ng/mL
Rat 10 mg/kg p.o. F 41.7 %
体内研究
(In Vivo)

CDK9-IN-40 (Compound 8e) (60 mg/kg，口服灌胃，每日1次，持续 7 天) 在 HCT116 异种移植小鼠模型中显示出强效体内抗肿瘤活性，60 mg/kg剂量下的肿瘤生长抑制率为 59.2%，无明显毒性体征[1]。

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

Animal Model: Four-week-old pathogen-free male Balb/c-nu mice were used to establish HCT116 xenograft models [1]
Dosage: 30 mg/kg, 60 mg/kg
Administration: Oral gavage (PO); Once daily; for 7 days; 4 days after cell injection
Result: Exhibited potent antitumor effects, suppressing tumor growth by 59.2% at a dose of 60 mg/kg per day.
分子量

422.55

Formula

C21H26N8S
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

CDK9-IN-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:

CDK9-IN-40CDKApoptosisCyclin dependent kinaseAntiproliferative activityCDK9Structure-activity relationshipTetrahydrothiazolopyridineInhibitorinhibitorinhibit

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：
CDK9-IN-40
目录号：
HY-176736
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