CVT-313Cdk2 inhibitor CAS# 199986-75-9 |
- LY2835219
Catalog No.:BCC1113
CAS No.:1231930-82-7
- Roscovitine (Seliciclib,CYC202)
Catalog No.:BCC1105
CAS No.:186692-46-6
- Nu 6027
Catalog No.:BCC1154
CAS No.:220036-08-8
- SNS-032 (BMS-387032)
Catalog No.:BCC1152
CAS No.:345627-80-7
- AT7519 Hydrochloride
Catalog No.:BCC1376
CAS No.:902135-91-5
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
Cas No. | 199986-75-9 | SDF | Download SDF |
PubChem ID | 6918386 | Appearance | Powder |
Formula | C20H28N6O3 | M.Wt | 400.47 |
Type of Compound | N/A | Storage | Desiccate at -20°C |
Synonyms | NG26 | ||
Solubility | DMSO : ≥ 100 mg/mL (249.71 mM) *"≥" means soluble, but saturation unknown. | ||
Chemical Name | 2-[2-hydroxyethyl-[6-[(4-methoxyphenyl)methylamino]-9-propan-2-ylpurin-2-yl]amino]ethanol | ||
SMILES | CC(C)N1C=NC2=C1N=C(N=C2NCC3=CC=C(C=C3)OC)N(CCO)CCO | ||
Standard InChIKey | NQVIIUBWMBHLOZ-UHFFFAOYSA-N | ||
Standard InChI | InChI=1S/C20H28N6O3/c1-14(2)26-13-22-17-18(21-12-15-4-6-16(29-3)7-5-15)23-20(24-19(17)26)25(8-10-27)9-11-28/h4-7,13-14,27-28H,8-12H2,1-3H3,(H,21,23,24) | ||
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
||
About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
||
Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. |
Description | cdk2 inhibitor (IC50 = 0.5 μM). Exhibits >8-fold selectivity for CDK2 over CDK1 and CDK4 (IC50 values are 4.2 and 215 μM, respectively). Inhibits proliferation rat neonatal aortic smooth muscle cells and a range of tumor cells lines in vitro. Inhibits restenosis in a rat carotid artery injury model. |
CVT-313 Dilution Calculator
CVT-313 Molarity Calculator
1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
1 mM | 2.4971 mL | 12.4853 mL | 24.9707 mL | 49.9413 mL | 62.4266 mL |
5 mM | 0.4994 mL | 2.4971 mL | 4.9941 mL | 9.9883 mL | 12.4853 mL |
10 mM | 0.2497 mL | 1.2485 mL | 2.4971 mL | 4.9941 mL | 6.2427 mL |
50 mM | 0.0499 mL | 0.2497 mL | 0.4994 mL | 0.9988 mL | 1.2485 mL |
100 mM | 0.025 mL | 0.1249 mL | 0.2497 mL | 0.4994 mL | 0.6243 mL |
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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.
- UCL 1684
Catalog No.:BCC7016
CAS No.:199934-16-2
- Chrysoeriol-7-O-glucoside
Catalog No.:BCN3796
CAS No.:19993-32-9
- DL-Alanyl-DL-Methionine
Catalog No.:BCC8950
CAS No.:1999-43-5
- RS 127445
Catalog No.:BCC1909
CAS No.:199864-87-4
- Isocudraniaxanthone B
Catalog No.:BCN6887
CAS No.:199851-52-0
- PD 166793
Catalog No.:BCC2376
CAS No.:199850-67-4
- Stattic
Catalog No.:BCC1176
CAS No.:19983-44-9
- 1-Actamido-3,5-dimethyladmantane
Catalog No.:BCC8449
CAS No.:19982-07-1
- Liguiritigenin-7-O-D-apiosyl-4'-O-D-glucoside
Catalog No.:BCN2840
CAS No.:199796-12-8
- LY 334370 hydrochloride
Catalog No.:BCC7559
CAS No.:199673-74-0
- Ro 61-8048
Catalog No.:BCC7619
CAS No.:199666-03-0
- CP 465022 hydrochloride
Catalog No.:BCC7520
CAS No.:199655-36-2
- ALX 5407 hydrochloride
Catalog No.:BCC7168
CAS No.:200006-08-2
- Benzyl 4-bromophenyl ketone
Catalog No.:BCC8868
CAS No.:2001-29-8
- Valinomycin
Catalog No.:BCC7671
CAS No.:2001-95-8
- H-Arg(Pbf)-OH
Catalog No.:BCC2866
CAS No.:200115-86-2
- H-D-Arg(Pbf)-OH
Catalog No.:BCC2872
CAS No.:200116-81-0
- SKF 38393 hydrobromide
Catalog No.:BCC6848
CAS No.:20012-10-6
- Boc-Arg(Pbf)-OH
Catalog No.:BCC3066
CAS No.:200124-22-7
- 3'-Methoxydaidzin
Catalog No.:BCN7720
CAS No.:200127-80-6
- Caulophylline hydriodide
Catalog No.:BCC8141
CAS No.:20013-22-3
- Isoscoparin
Catalog No.:BCN7845
CAS No.:20013-23-4
- Pyrocurzerenone
Catalog No.:BCN4067
CAS No.:20013-75-6
- Dehydrochromolaenin
Catalog No.:BCN4072
CAS No.:20013-76-7
CVT-313, a specific and potent inhibitor of CDK2 that prevents neointimal proliferation.[Pubmed:9360999]
J Biol Chem. 1997 Nov 14;272(46):29207-11.
The activity of cyclin-dependent kinase 2 (CDK2) is essential for progression of cells from G1 to the S phase of the mammalian cell cycle. CVT-313 is a potent CDK2 inhibitor, which was identified from a purine analog library with an IC50 of 0.5 microM in vitro. Inhibition was competitive with respect to ATP (Ki = 95 nM), and selective CVT-313 had 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 was required for half-maximal inhibition of the enzyme activity. In cells exposed to CVT-313, hyperphosphorylation of the retinoblastoma gene product was inhibited, and progression through the cell cycle was arrested at the G1/S boundary. The growth of mouse, rat, and human cells in culture was also inhibited by CVT-313 with the IC50 for growth arrest ranging from 1.25 to 20 microM. To evaluate the effects of CVT-313 in vivo, we tested this agent in a rat carotid artery model of restenosis. A brief intraluminal exposure of CVT-313 to a denuded rat carotid artery resulted in more than 80% inhibition of neointima formation. These observations suggest that CVT-313 is a promising candidate for evaluation in other disease models related to aberrant cell proliferation.