582315-72-8 Usage
Description
BMS-265246 is a pyrazolopyridine-based compound that acts as a potent and selective inhibitor of cyclin-dependent kinases (cdk) 2/cyclinE, cdk1/cyclinB, and cdk4/cyclinD. It is designed to target and disrupt the activity of these protein complexes, which play a crucial role in regulating cell cycle progression and are often dysregulated in various diseases, including cancer.
Uses
Used in Pharmaceutical Industry:
BMS-265246 is used as a therapeutic agent for the treatment of cancer. Its ability to inhibit multiple cdk/cyclin complexes makes it a promising candidate for targeting the dysregulated cell cycle machinery in cancer cells, potentially leading to the inhibition of tumor growth and progression.
Used in Research and Development:
BMS-265246 is also used as a research tool in the field of cell biology and oncology. It helps researchers understand the role of cdk/cyclin complexes in cell cycle regulation and their involvement in the development and progression of various cancers. This knowledge can be applied to the development of novel therapeutic strategies and the identification of potential biomarkers for cancer diagnosis and prognosis.
Used in Drug Discovery and Development:
BMS-265246 serves as a lead compound in the development of new drugs targeting the cell cycle machinery. Its potent and selective inhibition of cdk/cyclin complexes can be leveraged to design and synthesize new molecules with improved pharmacological properties, such as better selectivity, potency, and reduced side effects. These new compounds can then be tested for their efficacy in preclinical and clinical studies, potentially leading to the development of novel cancer treatments.
Biological Activity
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. bioorgmed 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.
Check Digit Verification of cas no
The CAS Registry Mumber 582315-72-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 5,8,2,3,1 and 5 respectively; the second part has 2 digits, 7 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 582315-72:
(8*5)+(7*8)+(6*2)+(5*3)+(4*1)+(3*5)+(2*7)+(1*2)=158
158 % 10 = 8
So 582315-72-8 is a valid CAS Registry Number.
582315-72-8Relevant articles and documents
1H-pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: Highly potent 2,6-difluorophenacyl analogues
Misra, Raj N.,Xiao, Hai-Yun,Rawlins, David B.,Shan, Weifang,Kellar, Kristen A.,Mulheron, Janet G.,Sack, John S.,Tokarski, John S.,Kimball, S. David,Webster, Kevin R.
, p. 2405 - 2408 (2003)
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 IC50=6 nM, CDK2/cycE IC50=9 nM). The 2,6-difluorophenyl substitution was cri
