中文名称: | CVT-313 | ||||
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英文名称: | CVT-313 | ||||
别名: | CDK CVT313;2,2'-((9-isopropyl-6-((4-methoxybenzyl)amino)-9H-purin-2-yl)azanediyl)bis(ethan-1-ol) | ||||
CAS No: | 199986-75-9 | 分子式: | C20H28N6O3 | 分子量: | 400.48 |
CAS No: | 199986-75-9 | ||||
分子式: | C20H28N6O3 | ||||
分子量: | 400.48 |
基本信息
产品编号:C10394 |
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产品名称:CVT-313 |
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CAS: |
199986-75-9 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
两年 |
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分子量 |
400.48 |
-20℃ |
一个月 |
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化学名: |
2,2'-((9-Isopropyl-6-((4-methoxybenzyl)amino)-9H-purin-2-yl)azanediyl)diethanol |
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Solubility (25°C) |
体外 |
DMSO |
80mg/mL (199.76mM) |
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Ethanol |
80mg/mL (199.76mM) |
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Water |
Insoluble |
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体内 |
现配现用 |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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。 |
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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: |
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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.
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细胞实验: |
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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. |
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
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )