General
Preferred name
BX-912
Synonyms
KIN001-175 ()
BX 912 ()
BX912 ()
P&D ID
PD011032
CAS
702674-56-4
Tags
available
drug candidate
Drug indication
Discovery agent
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 BX-912 is a direct, selective, and ATP-competitive PDK1 inhibitor (IC50=26 nM). BX-912 blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induces apoptosis[1].
PRICE 139
DESCRIPTION BX-912 is a potent, ATP-competitive and specific inhibitor of 3-phosphoinositide dependent protein kinase 1 (PDK1). The discovery of BX-912 is described in and is covered by patent WO2004048343 . The PDK1/Akt signaling pathway plays a key role in cancer cell growth, survival, and tumour angiogenesis and represents a promising target for oncology therapeutics . (GtoPdb)
DESCRIPTION BX-912 is a selective inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1) with IC50 of 12 nM; >10 fold selectivity over PKA, PKC, C-Kit, EGFR etc. (BOC Sciences Bioactive Compounds)
DESCRIPTION BX-912 is a specific inhibitor of 3-Phosphoinositide-dependent Kinase-1 (PDK1, IC50: 12 nM). The selectivity of BX-912 is more 10 fold than C-Kit, EGFR, PKA, PKC etc. (TargetMol Bioactive Compound Library)
Compound Sets
17
AdooQ Bioactive Compound Library
A11149
Axon Medchem Screening Library
1130
BOC Sciences Bioactive Compounds
bx912-cas-702674-56-4-item-84-131162
Cayman Chemical Bioactives
14708
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
DMZA45C
EU-OPENSCREEN Bioactive Compound Library
EOS101345
Guide to Pharmacology
8007
JUMP-MOA Compound Set
11754511
LINCS compound set
10055-101
Mcule NIBR MoA Box Subset
MCULE-7057328830
MedChem Express Bioactive Compound Library
HY-11005
Novartis Chemogenetic Library (NIBR MoA Box)
Selleckchem Bioactive Compound Library
bx-912
TargetMol Bioactive Compound Library
T1837
Welcome Trust Cancer Drugs
222
External IDs
23
Properties
(calculated by RDKit )
Molecular Weight
470.12
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
4
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
3
cLogP
3.99
TPSA
110.86
Fraction CSP3
0.3
Chiral centers
0.0
Largest ring
6.0
QED
0.41
QED
0.41
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Pathway
PI3K signaling
Angiogenesis
Cell Cycle/Checkpoint
PI3K/Akt/mTOR signaling
Tyrosine Kinase/Adaptors
PI3K/Akt/mTOR
Target
PDK1 (PDPK1)
Apoptosis
CDK2/CyclinE
CHK1
PDK1
PKA
VEGFR2 (KDR)
CDK2, CHEK1, GSK3B, KDR, PDK1, PDPK1
PDK1 inhibitor
PDK
PDK-1
Member status
member
MOA
PKB beta/Akt2 Inhibitors
pyruvate dehydrogenase kinase inhibitor
Source data