General
Preferred name
PHA-767491
Synonyms
PHA 767491 hydrochloride ()
PHA767491 ()
CAY10572 ()
PHA 767491 ()
PHA767491 HCl ()
CAY10572 HCl ()
PHA-767491 HCl ()
CAY-10572 hydrochloride ()
Cdc7/Cdk9 Inhibitor ()
PHA-767491 (hydrochloride) ()
CAY10572, NMS 1116354 ()
PHA-767491 hydrochloride ()
compound 8 [PMID: 17480064] ()
P&D ID
PD010690
CAS
845714-00-3
942425-68-5
845538-12-7
Tags
available
drug candidate
Drug indication
Discovery agent
Drug Status
investigational
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 PHA-767491 hydrochloride is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
PRICE 35
DESCRIPTION PHA-767491 hydrochloride (CAY-10572 hydrochloride) is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-?? and CDK1/2, 50-fold selectivity against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1.
DESCRIPTION Compound 8 is reported in as an inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MK-2; MAPKAPK2). Montagnoli et al. (2008) report the antitumour activity of this compound . (GtoPdb)
DESCRIPTION PHA-767491 is a dual Cdc7/Cdk9 inhibitor, with IC50s of 10 nM and 34 nM, respectively.
PRICE 41
DESCRIPTION MRN-ATM pathway inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION MK2 inhibitor; also inhibits cdc7/cdk9 (Tocriscreen Plus)
DESCRIPTION PHA-767491 hydrochloride is a potent, ATP-competitive dual Cdc7/Cdk9 inhibitor, which prevents initiation of DNA replication. It inhibits cell proliferation in a variety of human cell lines and induces apoptosis in a p53-independent manner in vivo. It also inhibits mitogen-activated protein kinase-activated protein kinase-2 (MK2). (BOC Sciences Bioactive Compounds)
DESCRIPTION PHA-767491 hydrochloride (CAY-10572 hydrochloride) is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1. (TargetMol Bioactive Compound Library)
DESCRIPTION PHA-767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication. (BOC Sciences Bioactive Compounds)
DESCRIPTION PHA-767491 (CAY10572) is a potent ATP-competitive dual Cdc7/CDK9 inhibitor with IC50 of 10 nM and 34 nM, respectively. (TargetMol Bioactive Compound Library)
Cell lines
20
Organisms
1
Compound Sets
21
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
CDK inhibitor database (CDKiDB)
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
Enamine Bioactive Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LINCS compound set
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
ZINC Tool Compounds
External IDs
37
Properties
(calculated by RDKit )
Molecular Weight
213.09
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
2
Rotatable Bonds
1
Ring Count
3
Aromatic Ring Count
2
cLogP
1.36
TPSA
57.78
Fraction CSP3
0.17
Chiral centers
0.0
Largest ring
6.0
QED
0.75
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Enzymes
Target
Cdc7
CDK
CDK1
CDK2
CDK9
GSK-3β
Apoptosis
CDK1, RPS6KB1
CDC7/CDK9 inhibitor
Primary Target
MK2
MOA
Inhibitor
Inhibitors of Signal Transduction Pathways
Cell Division Cycle 7-Related Protein Kinase (CDC7) Inhibitors
CDC inhibitor
Member status
member
Pathway
Cell Cycle/Checkpoint
GPCR/G protein
PI3K/Akt/mTOR signaling
Stem Cells
Cell Cycle/DNA Damage
Source data