1. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR
  2. CDK GSK-3
  3. CDK7-IN-20

CDK7-IN-20 是一种有效的、选择性的、不可逆的 CDK7 (CDK) 抑制剂,IC50 值为 4 nM。CDK7-IN-20 对 CDK7 的选择性超过 CDK1、CDK2、CDK3、CDK5、CDK6、CDK9 和 CDK12 的 206 倍以上。CDK7-IN-20 具有用于常染色体显性多囊肾病 (ADPKD) 研究的潜力。

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

CDK7-IN-20 Chemical Structure

CDK7-IN-20 Chemical Structure

CAS No. : 3034210-97-1

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK7-IN-20 is a potent, selective and irreversible CDK7 (CDK) inhibitor with an IC50 value of 4 nM. CDK7-IN-20 displays >206-fold selectivity for CDK7 over CDK1, CDK2, CDK3, CDK5, CDK6, CDK9 and CDK12 . CDK7-IN-20 has the potential for autosomal dominant polycystic kidney disease (ADPKD) research[1].

IC50 & Target[1]

CDK7

4 nM (IC50)

CDK1

3375 nM (IC50)

CDK2

823 nM (IC50)

CDK3

1837 nM (IC50)

CDK5

>10,000 nM (IC50)

CDK6

950 nM (IC50)

CDK9

526 nM (IC50)

CDK12

>10,000 nM (IC50)

GSK3β

148 nM (IC50)

体外研究
(In Vitro)

In Madin-Darby canine kidney (MDCK) cells, CDK7-IN-20 (Compound B2; 1-3 μM; from day 4 to day 12) shows high potency to inhibit cyst growth and exhibited lower cytotoxicity than THZ1[1].

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

体内研究
(In Vivo)

CDK7-IN-20 (Compound B2; 5 mg/kg; s.c; once daily; for 6 days) significantly reduces the kidney size and cyst formation of the ADPKD mice. The protein expression of AMPD3 could be significantly down-regulated by CDK7-IN-20 in the cyst-lining epithelial cells of the ADPKD mouse kidney[1].
ADME Profiles of CDK7-IN-20 (Compound B2)a[1].

CDK7-IN-20 (Compound B2)
parameters i.v. 5 mg/kg s.c. 5 mg/kg
AUClast (h·ng/mL) 26,937 17,280
AUCIFN_obs (h·ng/mL) 31,698 17,411
t1/2 (h) 17.8 3.4
Tmax (h) 0.5
Cmax (h) 3806
Cl_obs (mL/min/kg) 2.80
Vss_obs (mL/kg) 1275
MRTIFN_obs (h) 10.2 4.8
F (%) 64.2
plasma protein binding (bound%)b >99
permeability of Caco-2 A to B Papp (10–6 cm/s)/B to A Papp (10–6 cm/s)/efflux ratioc <0.133/6.370/>48.0
aThree ICR mice were used for each group. The data are expressed as mean values.
bPlasma from mouse. PPB was tested at 1 and 10 μM substrate concentrations.
bCaco-2 membrane permeability at 10 μM substrate concentrations. The value of 0.133 was determined by quantitative limit (1.0 nM)[1].

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

Animal Model: Neonatal Pkd1flox/flox:Ksp-Cre mice[1]
Dosage: 5 mg/kg
Administration: Subcutaneous administration; once daily; for 6 days
Result: Significantly reduced the kidney size and cyst formation of the ADPKD mice.
分子量

518.57

Formula

C30H26N6O3

CAS 号
非同位 CAS

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
  • 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.

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:
CDK7-IN-20
目录号:
HY-151878
需求量: