General
Preferred name
PD0166285
Synonyms
PD 166285 dihydrochloride ()
PD-0166285 ()
PD-166285 ()
PD166285 ()
Heparin-Cantithrombin III ()
SB-601273 ()
PD-0166285 HYDROCHLORIDE ()
TCMDC-140940 ()
Pd-0166285 dihydrochloride ()
PD 166285 ()
P&D ID
PD049371
CAS
212391-63-4
185039-89-8
Tags
available
obsolete probe
drug candidate
Drug indication
Discovery agent
Drug Status
investigational
Max Phase
1.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
PD166285 was originally reported as a tyrosine kinase inhibitor , and has subsequently been identified as an inhibitor of Wee1 and Myt1 (PKMYT1) , two cyclin-dependent kinase (CDK) inhibitory kinases involved in regulating the cell cycle.
(GtoPdb)
DESCRIPTION
PD0166285, a substrate of P-gp, is a WEE1 inhibitor and a weak Myt1 inhibitor with IC50 values of 24 and 72 nM, respectively. PD0166285 exhibits an IC50 of 3.433 ¦ÌM for Chk1[1].
PRICE
214
DESCRIPTION
PD0166285 is a potent Wee1 inhibitor and Chk1 inhibitor with activity at nanomolar concentrations. This G2 checkpoint abrogation by PD0166285 was demonstrated to kill cancer cells, there at a toxic highest dose of 0.5 muM in some cell lines for exposure periods of no longer than 6 hours. The deregulated cell cycle progression may have ultimately damaged the cancer cells. We herein report one of the mechanism by which PD0166285 leads to cell death in the B16 mouse melanoma cell line.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Selective TrioN RhoGEF activity inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Potent Src inhibitor; also inhibits FGFR1, PDGFRbeta and Wee1
(Tocriscreen Plus)
DESCRIPTION
PD 166285, a novel protein tyrosine kinase inhibitor of a new structural class, is a potent inhibitor of the tyrosine kinases c-Src, Flg (fibroblast growth factor receptor 1, FGFR1), and PDGFRβ (platelet-derived growth factor receptor β) (IC50 values are 8.4, 39.3 and 98.3 nM respectively). PD 166285 also inhibits the checkpoint kinases Wee1 and MYT1 (Myt1), abolishes Cdc2 phosphorylation in numerous tumor cell lines, and abrogates the G2 checkpoint.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
8
Organisms
0
Compound Sets
22
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Chemical proteomics reveals the target landscape of 1,000 kinase inhibitors
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
Enamine Bioactive Compounds
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Obsolete Compounds
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
35
Molecular Weight
511.15
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
1
Rotatable Bonds
9
Ring Count
4
Aromatic Ring Count
4
cLogP
5.77
TPSA
72.28
Fraction CSP3
0.27
Chiral centers
0.0
Largest ring
6.0
QED
0.31
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target Type
Enzymes
Target
Apoptosis
CHK1
Myt1
WEE1
EGFR, FGFR1, PDGFRB, PKMYT1, SRC, WEE1
Apoptosis related,Chk,Wee1
Primary Target
Src Kinases
MOA
Inhibitor
Src inhibitor
Pathway
Cell Cycle/Checkpoint
Cell Cycle/DNA Damage
Solubility
DMSO to 100 mM
Soluble in DMSO
Source data
