BMS265246

CDK1/2 inhibitor,potent and selective CAS# 582315-72-8

BMS265246

Catalog No. BCC3741----Order now to get a substantial discount!

Product Name & Size Price Stock
BMS265246:5mg $181.00 In stock
BMS265246:10mg $308.00 In stock
BMS265246:25mg $724.00 In stock
BMS265246:50mg $1267.00 In stock
Related Products

Quality Control of BMS265246

Number of papers citing our products

Chemical structure

BMS265246

3D structure

Chemical Properties of BMS265246

Cas No. 582315-72-8 SDF Download SDF
PubChem ID 5329775 Appearance Powder
Formula C18H17F2N3O2 M.Wt 345.34
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in DMSO
Chemical Name (4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone
SMILES CCCCOC1=C2C=NNC2=NC=C1C(=O)C3=C(C=C(C=C3F)C)F
Standard InChIKey SCFMWQIQBVZOQR-UHFFFAOYSA-N
Standard InChI InChI=1S/C18H17F2N3O2/c1-3-4-5-25-17-11(8-21-18-12(17)9-22-23-18)16(24)15-13(19)6-10(2)7-14(15)20/h6-9H,3-5H2,1-2H3,(H,21,22,23)
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.

Biological Activity of BMS265246

DescriptionPotent cdk1/2 inhibitor (IC50 values are 6, 9 and 230 nM for cdk1, cdk2 and cdk4, respectively). Inhibits proliferation of HCT-116 colon cancer cells in vitro.

BMS265246 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

BMS265246 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of BMS265246

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.8957 mL 14.4785 mL 28.957 mL 57.9139 mL 72.3924 mL
5 mM 0.5791 mL 2.8957 mL 5.7914 mL 11.5828 mL 14.4785 mL
10 mM 0.2896 mL 1.4478 mL 2.8957 mL 5.7914 mL 7.2392 mL
50 mM 0.0579 mL 0.2896 mL 0.5791 mL 1.1583 mL 1.4478 mL
100 mM 0.029 mL 0.1448 mL 0.2896 mL 0.5791 mL 0.7239 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.

Organizitions Citing Our Products recently

 
 
 

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
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on BMS265246

BMS265246 is a potent and selective inhibitor for CDK1 and CDK2 (IC50= 6 nM and 9 nM)

Cyclin-dependent kinases (CDK) are a group of serine/threonine kinases. They are activated by coupling to cyclin and participate in the regulation of cell cycle.

BMS265246 inhibited the Cdk4/cycD activity and prevented A2780 Cytox (IC50 = 0.23 μM and 0.76 μM) [1]. In HCT-116 cells, BMS-265246 blocked the cell proliferation (EC50= 0.293 μm—0.492 μm). Following the treatment of BMS-265246, low DNA intensity, large round nuclei and 4N DNA content were observed in the dominant cell population –G2 arrested cells. [2]

References:
1. Misra RN, Xiao Hy, Rawlins DB et al.  1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.  Bioorg
Med Chem Lett.  2003 Jul 21;13(14):2405-8.
2. Sutherland JJ, Low J, Blosser W et al.  A robust high-content imaging approach for probing the mechanism of action and phenotypic outcomes of cell-cycle modulators. Mol Cancer Ther. 2011 Feb;10(2):242-54.

Featured Products
New Products
 

References on BMS265246

1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.[Pubmed:12824044]

Bioorg Med Chem Lett. 2003 Jul 21;13(14):2405-8.

Structure-activity studies of 1H-pyrazolo[3,4-b]pyridine 1 have resulted in the discovery of potent CDK1/CDK2 selective inhibitor 21h, BMS-265246 (CDK1/cycB IC(50)=6 nM, CDK2/cycE IC(50)=9 nM). The 2,6-difluorophenyl substitution was critical for potent inhibitory activity. A solid state structure of 21j, a close di-fluoro analogue, bound to CDK2 shows the inhibitor resides coincident with the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone.

Description

Potent cdk1/2 inhibitor,BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4.

Keywords:

BMS265246,582315-72-8,Natural Products,Cyclin-Dependent Kinases, buy BMS265246 , BMS265246 supplier , purchase BMS265246 , BMS265246 cost , BMS265246 manufacturer , order BMS265246 , high purity BMS265246

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: