General
Preferred name
SNS-314
Synonyms
SNS 314 mesylate ()
SNS-314 Mesylate ()
SNS-314 (mesylate) ()
Sns 314 ()
P&D ID
PD005309
CAS
1057249-41-8
1146618-41-8
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Drug Status
investigational
Max Phase
Phase 1
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION SNS-314 is an inhibitor of Aurora kinases A and B . CHEMBL482767 represents an alternative tautomer of the compound. (GtoPdb)
MOA The process of cell division, or mitosis, plays a critical role in the uncontrolled proliferation that is a hallmark of cancer. During mitosis, a cell aligns duplicate copies of its DNA along a mitotic spindle and subdivides itself through a process called cytokinesis, creating two identical daughter cells. This process is often poorly regulated in cancer, leading to rapid proliferation and tissue growth. Aurora kinases (A, B, and C) play important, though differentiated, roles in mitosis. Aurora A controls the formation of the spindle assembly, while Aurora B ensures that the DNA is appropriately aligned and that cytokinesis proceeds successfully. Less is known about Aurora C, though it is thought to serve many of the same functions as Aurora B. Elevated expression of Aurora A has been detected in a high percentage of colon, breast, ovarian, gastric, and pancreatic tumors. Aurora B and C are also expressed at high levels in primary tumors.; ; Given the central roles of all three Aurora kinases in regulating mitosis and the association between their overexpression and tumorigenesis, they are being evaluated as potential targets in cancer therapy. SNS-314 is a potent inhibitor of all 3 Aurora kinases. Cells treated with SNS-314 make additional copies of their DNA, but are unable to create functional spindle assemblies or replicate. As a result, these cells are unable to progress, and ultimately die by a variety of mechanisms. Since most normal cells are not undergoing mitosis in their normal settings, SNS-314 is expected to affect only highly proliferating tissues, particularly tumor tissues. SNS-314 is being tested in a Phase 1 trial in patients with advanced solid tumor malignancies.
DESCRIPTION p38 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Potent pan-Aurora kinase inhibitor (Tocriscreen Plus)
DESCRIPTION SNS-314 Mesylate is a potent and selective inhibitor of Aurora A, Aurora B and Aurora C with IC50 of 9 nM, 31 nM, and 3 nM, respectively. It is less potent to Trk A/B, Flt4, Fms, Axl, c-Raf and DDR2. Phase 1. (BOC Sciences Bioactive Compounds)
DESCRIPTION SNS-314 is a synthetic small molecule Aurora kinase (AK) inhibitor with potential antineoplastic activity. Aurora kinase inhibitor SNS-314 selectively binds to and inhibits AKs A and B, which may result in the inhibition of cellular division and proliferation in tumor cells that overexpress AKs. AKs are serine-threonine kinases that play essential roles in mitotic checkpoint control during mitosis. (BOC Sciences Bioactive Compounds)
Cell lines
1
Organisms
0
Compound Sets
19
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
External IDs
36
Properties
(calculated by RDKit )
Molecular Weight
430.04
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
3
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
4
cLogP
5.1
TPSA
91.83
Fraction CSP3
0.11
Chiral centers
0.0
Largest ring
6.0
QED
0.4
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Enzymes
Targets
AURKA,AURKB,AURKC
Pathway
Cell Cycle/Checkpoint
Chromatin/Epigenetic
Cell Cycle/DNA Damage
Epigenetics
Target
Aurora A
Aurora B
Aurora C
AURKA, AURKB, AURKC
Aurora inhibitor
Aurora Kinase
Primary Target
Aurora Kinases
MOA
Inhibitor
Aurora Kinase inhibitor
Therapeutic Class
Anticancer Agents
Source data