BMS265246|CDK1/2 inhibitor,potent and selective|CAS# 582315-72-8

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Size	Price	Stock
10mM (in 1mL DMSO)	$209.00	In stock
5mg	$189.00	In stock
10mg	$259.00	In stock

Publications citing ApexBio Products

Nature.
2016 Apr 21;532(7599):398-401.

Nature.
2015 Aug 20;524(7565):309-14.

Cell.
2015 Aug 27;162(5):987-1002.

Cell.
2015 Feb 12;160(4):729-44.

Immunity.
2016 Jan 19;44(1):88-102

Nat Cell Biol.
2015 May;17(5):627-38.

Nat Neurosci.
2015 Oct;18(10):1464-73.

Nat Commun.
2016 Feb 1;7:10492.

J Cell Biol.
2016 Apr 11;213(1):109-25.

Cell Host Microbe.
2016 Jul 13;20(1):13-24.

Proc Natl Acad Sci U S A.
2016 Mar 8;113(10):2585-90.

Proc Natl Acad Sci U S A.
2015 Jun 30;112(26):E3365-73.

Proc Natl Acad Sci U S A.
2015 Jul 28;112(30):9412-7.

Autophagy.
2016 Jul 2;12(7):1129-52.

Cancer Res canres.
2946.2015.

Elife.
2016 Jan 14;5. pii: e12203.

Nucleic Acids Res.
2016 Feb 18;44(3):e2.

EMBO Rep.
2015 Sep;16(9):1114-30.

Oncogene.
2016 Mar 21.

Cell Rep.
2015 Sep 29;12(12):1986-96.

Cell Death Differ.
2016 Jun;23(6):1026-37.

Cell Death Differ.
2016 Jan;23(1):76-88.

Diabetes Obes Metab.
2015 Apr;17(4):403-13.

Oncotarget.
2015 Jan 20;6(2):1171-89.

J Neurosci.
2015 Sep 23;35(38):13244-56.

Sci Signal.
2014 Dec 23;7(357):ra122.

Mol Ther.
2015 Sep;23(9):1475-85.

J Nucl Med.
2016 Feb;57 Suppl 1:75S-80S.

Cardiovasc Res.
2015 Apr 1;106(1):153-62.

Cell Mol Life Sci.
2015 Nov;72(22):4399-407.

Anal Chem.
2015;87(10):5046-9.

Cancer Lett.
2016 Apr 28;374(1):1-11.

Quality Control

Quality Control & MSDS

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Purity = 98.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

Chemical structure

Biological Activity

Description	BMS-265246 is a potent and selective inhibitor of CDK1 and CDK2 with IC50 values of 6 nM and 9 nM, respectively.
Targets	CDK1/CyclinB	CDK2/CyclinE	CDK4/CyclinD
IC50	6 nM	9 nM	230 nM

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Chemical Properties

Cas No.	582315-72-8	SDF	Download SDF
Chemical Name	(4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)-(2,6-difluoro-4-methylphenyl)methanone
Canonical SMILES	CCCCOC1=C2C=NNC2=NC=C1C(=O)C3=C(C=C(C=C3F)C)F
Formula	C₁₈H₁₇F₂N₃O₂	M.Wt	345.34
Solubility	Soluble in DMSO > 10 mM	Storage	Store at -20°C
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.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

Background

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.