CVT-313
(Synonyms: CVT 313;NG 26;CVT313;NG26;NG-26) 目录号 : GC18028
A Cdk2 inhibitor
Cas No.:199986-75-9
Sample solution is provided at 25 µL, 10mM.
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CVT-313 is a potent inhibitor of cyclin-dependent kinase 2 (CDK2) with IC50 value of 0.5 μM [1].
CDK2 is a serine/threonine kinase that is essential for the G1-S phase during cell division. CDK2 is an important target for prevention of aberrant cell proliferation [1].
In MRC-5 cells, CVT-313 inhibited Rb hyperphosphorylation in a time-dependant way and the cell cycle was arrested at the G1/S phase. Also, CVT-313 inhibited the growth of mouse, rat and human cells with IC50 values from 1.25 to 20 mM [1]. In human diffuse large B-cell lymphoma (DLBCL) cells, CVT-313 reduced CDK2-mediated phosphorylation of the retinoblastoma gene product (Rb) on T821. Also, CVT-313 reduced the anti-apoptotic factor Myeloid cell leukemia-1 (Mcl-1) and induced apoptosis [2].
In the injured rat carotid artery model of restenosis, CVT-313 (1.25 mg/kg) reduced neointima formation by 80%. Moreover, Treatment animals with CVT-313, the neointimal areas were inhibited by at least 70%. These suggested that CDK2 was an antiproliferative target and CVT-313 is an ideal candidate for the treatment of proliferative diseases [1].
References:
[1]. Brooks EE, Gray NS, Joly A, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation. J Biol Chem, 1997, 272(46): 29207-29211.
[2]. Faber AC, Chiles TC. Inhibition of cyclin-dependent kinase-2 induces apoptosis in human diffuse large B-cell lymphomas. Cell Cycle, 2007, 6(23): 2982-2989.
| Cell experiment [1,2]: | |
|
Cell lines |
Human DLBCL cells |
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Preparation method |
The solubility of this compound in DMSO is >20 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
25 μM, 24 hr |
|
Applications |
CVT-313 inhibited cdk2 in several human DLBCL cells. Incubation of DLBCL cells with 25 μM CVT-313 reduced phosphorylation of endogenous Rb on Thr821. CVT-313 (48 and 72 hr) induced cell apoptosis in human DLBCL cells in a time-dependent manner. CVT-313 treatment did not result in cell cycle arrest at 20 hr or at 48 hr. Treatment of LY3, LY8 cells and LY18 cells with CVT-313 led to parallel changes in XIAP and Mcl-1 mRNA levels. In normal and tumor human/murine cell lines, CVT-313 inhibited cell proliferation with the IC50 ranged from 1.25 to 20 μM. CVT-313 (12.5 μM, 18 h) induced cell arrest at the G1/S and G2/M boundary. In nonsynchronized MRC-5 cells, treatment with CVT-313 (6.25 μM) for 36 h induced a 2 N DNA content. Treatment with CVT-313 (6.25 μM) for 4 or 8 h after serum stimulation inhibited Rb hyperphosphorylation. |
| Animal experiment [2]: | |
|
Animal models |
Injured rat carotid artery model of restenosis |
|
Dosage form |
0.75 and 0.25 mg/kg |
|
Application |
In the injured rat carotid artery model of restenosis, lower doses of CVT-313 (0.75 and 0.25 mg/kg) were less efficacious, reducing mean neointimal area by about 30%, whereas the lowest dose tested (0.025 mg/kg) did not achieve any significant reduction in neointimal area. Treatment with CVT-313 for 14 days blocked restenosis in the rat carotid model. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Faber A C, Chiles T C. Inhibition of cyclin-dependent kinase-2 induces apoptosis in human diffuse large B-cell lymphomas[J]. Cell Cycle, 2007, 6(23): 2982-2989. [2]. Brooks E E, Gray N S, Joly A, et al. CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation[J]. Journal of Biological Chemistry, 1997, 272(46): 29207-29211. | |
| Cas No. | 199986-75-9 | SDF | |
| 别名 | CVT 313;NG 26;CVT313;NG26;NG-26 | ||
| 化学名 | 2-[2-hydroxyethyl-[6-[(4-methoxyphenyl)methylamino]-9-propan-2-ylpurin-2-yl]amino]ethanol | ||
| Canonical SMILES | CC(C)N1C=NC2=C1N=C(N=C2NCC3=CC=C(C=C3)OC)N(CCO)CCO | ||
| 分子式 | C20H28N6O3 | 分子量 | 400.47 |
| 溶解度 | ≥ 20 mg/mL in DMSO, ≥ 51.1 mg/mL in EtOH with gentle warming | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4971 mL | 12.4853 mL | 24.9707 mL |
| 5 mM | 0.4994 mL | 2.4971 mL | 4.9941 mL |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4971 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet