中文名称: CVT-313
英文名称: CVT-313
CAS No: 199986-75-9
分子式: C20H28N6O3
分子量: 400.48
C10394 CVT-313 ≥98%(HPLC) (psaitong)
包装规格:
5mg 10mg 50mg in glass bottle
溶解性:
溶于DMSO(≥100mg/mL)
产品描述:

基本信息

产品编号:C10394

产品名称:CVT-313

CAS:

199986-75-9

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C20H28N6O3

溶于液体

-80℃

两年

分子量

400.48

-20℃

一个月

化学名: 

2,2'-((9-Isopropyl-6-((4-methoxybenzyl)amino)-9H-purin-2-yl)azanediyl)diethanol

 

Solubility (25°C)

 

体外

DMSO

80mg/mL (199.76mM)

Ethanol

80mg/mL (199.76mM)

Water

Insoluble

体内

现配现用

 

1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。

 

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.4971mL

12.4853mL

24.9707mL

5mM

0.4994mL

2.4971mL

4.9941mL

10mM

0.2497mL

1.2485mL

2.4971mL

50mM

0.0499mL

0.2497mL

0.4994mL

 

 

生物活性

产品描述

一种有效的选择性的CDK2抑制剂,可防止内膜增生,IC50:0.5μM。

靶点/IC50

cdk2/cyclin A

0.5μM (IC50)

Cdk1/cyclin B 4.2μM (IC50)

Cdk4/cyclin D1 215μM (IC50)

 

体外研究

CVT-313 (Cdk2 Inhibitor III) has been shown to inhibit other kinases, but at much higher IC50 values, i.e., CDK1 (IC50=4.2μM),CDK4 D1 (IC50=215μM), and MAPK/PKA/PKC (IC50>1.25mM), compared to CDK2 (IC50=0.5μM). CVT-313 has been shown to have profound effects on cell proliferation at concentrations of 5-20μM. CVT-313 is a potent CDK2 inhibitor, which is identified from a purine analog library with an IC50 of 0.5μM in vitro. Inhibition is competitive with respect to ATP (Ki=95nM),and selective CVT-313 has no effect on other, nonrelated ATP-dependent serine/threonine kinases. When added to CDK1 or CDK4, a 8.5- and 430-fold higher concentration of CVT-313 is required for half-maximal inhibition of the enzyme activity.Using normal and tumor human/murine cell lines, the effects of CVT-313 on cell proliferation is measured. The IC50 for growth inhibition ranged from 1.25 to 20μM.

 

推荐实验方法(仅供参考)

激酶实验:

Kinase Assay

For kinase assays, purified CDC5L(295-795)-His6 is mixed with [γ-32P]ATP, COS-7 cell extract, and incubated in 100μL 20mM HEPES, pH 7.5, 50mM NaCl, 2mM MnCl2, 10mM MgCl2, 0.5% NP-40, 0.5mM PMSF, 5mM benzamidine hydrochloride, 5mM NaF, 1mM NaVO3 and the specific inhibitor at 30°C for 10 minutes. Cell extract as a source of kinase activity is prepared from subconfluent, serum-stimulated COS-7 cells lysed in 20mM HEPES-NaOH, pH 7.5, 50mM NaCl, 1% Triton X-100, 10% glycerol, protease and phosphotase inhibitors. Phosphorylated proteins are separated by electrophoresis in 15% polyacrylamide-SDS gels. Specific inhibitors included 20μM staurosporine, 10μM genistein, 1μM CVT-313, 10μM Rp-MBcAMPS and 50μM PD98059.

 

 

细胞实验:

 

Cell Assay

MRC-5 cells are grown in Dulbecco’s modified Eagle’s medium containing 5% fetal calf serum. CVT313 (0, 5, 10, 15μM) is added to exponentially growing cells in tissue culture. Cell population is measured. Proliferation assays are carried out using the nonradioactive CellTiter 96 kit after 48-h exposure. For FACS analysis of DNA content, cells are trypsinized, fixed in 70% ice-cold ethanol, and treated with 0.1mg/mL RNase A and 40μg/mL propidium iodide for 1 h at 37°C.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

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稀释公式

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  • * = *

连续稀释计算器方程

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  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):