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CVT-313

CVT-313

产品编号 T3195   CAS 199986-75-9
别名: CVT 313, Cdk2 Inhibitor III, CVT313, NG26

CVT-313 (NG26) 是一种有效的、选择性的、可逆的和 ATP 竞争性抑制剂,可抑制 CDC5L 磷酸化,对 CDK2的 IC50为 0.5 μM。

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CVT-313 Chemical Structure
CVT-313, CAS 199986-75-9
规格 价格/CNY 货期 数量
1 mg ¥ 273 现货
2 mg ¥ 383 现货
5 mg ¥ 678 现货
10 mg ¥ 987 现货
25 mg ¥ 1,930 现货
50 mg ¥ 3,570 现货
100 mg ¥ 4,970 现货
1 mL * 10 mM (in DMSO) ¥ 691 现货
千万补贴 助力科研
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产品目录号及名称: CVT-313 (T3195)
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纯度: 97.82%
纯度: 97.46%
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生物活性
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参考文献
产品描述 CVT-313 (NG-26) is a potent, selective, reversible, and ATP-competitive inhibitor.
靶点活性 CDK2:0.5 μM
体外活性 CVT-313 has been shown to inhibit other kinases, but at much higher IC50 values, i.e., CDK1 (IC50=4.2 μM), CDK4 D1 (IC50=215 μM), and MAPK/PKA/PKC (IC50>1.25 mM), compared to CDK2 (IC50=0.5 μM). CVT-313 has been shown to have profound effects on cell proliferation at concentrations of 5-20 μM[1]. CVT-313 is a potent CDK2 inhibitor, which is identified from a purine analog library with an IC50 of 0.5 μM in vitro. Inhibition is competitive with respect to ATP (Ki=95 nM), 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 20 μM[2].
激酶实验 For kinase assays, purified CDC5L(295-795)-His6 is mixed with [γ-32P]ATP, COS-7 cell extract, and incubated in 100 μL 20 mM HEPES, pH 7.5, 50 mM NaCl, 2 mM MnCl2, 10 mM MgCl2, 0.5% NP-40, 0.5 mM PMSF, 5 mM benzamidine hydrochloride, 5 mM NaF, 1 mM 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 20 mM HEPES-NaOH, pH 7.5, 50 mM 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 20 μM staurosporine, 10 μM genistein, 1 μM CVT-313, 10 μM Rp-MB-cAMPS and 50 μM PD98059[1].
细胞实验 CVT313 is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. MRC-5 cells are grown in Dulbecco's modified Eagle's medium containing 5% fetal calf serum. CVT313 (0, 5, 10, 15 μM) 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 0.1 mg/mL RNase A and 40 μg/mL propidium iodide for 1 h at 37°C[2].
别名 CVT 313, Cdk2 Inhibitor III, CVT313, NG26
分子量 400.47
分子式 C20H28N6O3
CAS No. 199986-75-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (124.85 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4971 mL 12.4853 mL 24.9707 mL 62.4266 mL
5 mM 0.4994 mL 2.4971 mL 4.9941 mL 12.4853 mL
10 mM 0.2497 mL 1.2485 mL 2.4971 mL 6.2427 mL
20 mM 0.1249 mL 0.6243 mL 1.2485 mL 3.1213 mL
50 mM 0.0499 mL 0.2497 mL 0.4994 mL 1.2485 mL
100 mM 0.025 mL 0.1249 mL 0.2497 mL 0.6243 mL

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TargetMol Library Books参考文献

1. Graub R, et al. Cell cycle-dependent phosphorylation of human CDC5 regulates RNA processing. Cell Cycle. 2008 Jun 15;7(12):1795-803. 2. Brooks EE, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem. 1997 Nov 14;272(46):29207-11.

TargetMol Library Books文献引用

1. Jiang L, Yu Y, Li Z, et al.BMS-265246, a Cyclin-Dependent Kinase Inhibitor, Inhibits the Infection of Herpes Simplex Virus Type 1.Viruses.2023, 15(8): 1642.
LRRK2 inhibitor 1 Purvalanol B JSH-150 GSK-3 inhibitor 4 (E/Z)-Zotiraciclib NU6027 NSC23005 PROTAC CDK9 Degrader-1

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 抗前列腺癌化合物库 临床前化合物库 抗心血管疾病化合物库 抗胰腺癌化合物库 NO PAINS 化合物库 已知活性化合物库 激酶抑制剂库 抗乳腺癌化合物库 抗癌化合物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

CVT-313 199986-75-9 Cell Cycle/Checkpoint CDK inhibit CVT 313 Cdk2 Inhibitor III CVT313 Cyclin dependent kinase NG-26 NG 26 NG26 Inhibitor inhibitor

 

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