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About This Item
Empirical Formula (Hill Notation):
C16H17Cl2N5O2
CAS Number:
Molecular Weight:
382.24
MDL number:
NACRES:
NA.21
Product Name
AT7519, ≥98% (HPLC), powder, CDK inhibitor
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Application
AT7519 may be used to study its effects on cell viability and proliferation, cell cycle, apoptosis and pyroptosis in human glioblastoma cells.
Biochem/physiol Actions
AT7519 is a potent and selective cyclin dependent kinase (CDK) inhibitor (CDK5-p35/CDK2-CycA/CDK4-CycD1/CDK1-CycB IC50 = 18/44/67/190 nM; IC50 >10 μM against Aurora A, IR, MEK1, PDK1, c-abl) with antiproliferative activity in cancer cultures (IC50 = 82 nM/HCT116, 350 nM/A2780) and antitumor efficacy in mice in vivo (86% inhibition of A2780 xenograft tumor growth post 8-day treatment at 7.5 mg/kg b.i.d. i.p., 87% inhibition of HCT116 xenograft tumor growth post 10-day treatment at 9.1 mg/kg b.i.d. i.p.).
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L Santo et al.
Oncogene, 29(16), 2325-2336 (2010-01-27)
Dysregulated cell cycling is a universal hallmark of cancer and is often mediated by abnormal activation of cyclin-dependent kinases (CDKs) and their cyclin partners. Overexpression of individual complexes are reported in multiple myeloma (MM), making them attractive therapeutic targets. In
Paul G Wyatt et al.
Journal of medicinal chemistry, 51(16), 4986-4999 (2008-07-29)
The application of fragment-based screening techniques to cyclin dependent kinase 2 (CDK2) identified multiple (>30) efficient, synthetically tractable small molecule hits for further optimization. Structure-based design approaches led to the identification of multiple lead series, which retained the key interactions
Matthew S Squires et al.
Molecular cancer therapeutics, 8(2), 324-332 (2009-01-29)
Cyclin-dependent kinases (CDK), and their regulatory cyclin partners, play a central role in eukaryotic cell growth, division, and death. This key role in cell cycle progression, as well as their deregulation in several human cancers, makes them attractive therapeutic targets
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