General
Preferred name
LGH-447
Synonyms
LGH447 ()
LGH 447 ()
PIM 447 ()
cpd 8 ()
5HZ ()
PIM447 ()
PIM-447 (dihydrochloride) ()
LGH447 dihydrochloride ()
PIM-447 ()
PIM KINASE INHIBITOR LGH447 ()
NVP-LGH477 ()
P&D ID
PD076541
CAS
1210608-43-7
1820565-69-2
Tags
available
probe
drug candidate
Drug indication
Multiple myeloma
Myelofibrosis
Drug Status
investigational
Max Phase
1.0
Probe info
Probe type
experimental probe
calculated probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Probe Miner (suitable probes)
Probe targets
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
COMMENT PIM-447 is a pan-PIM 1, 2 and 3 kinase inhibitor that demonstrates potent biochemical activity and good selectivity in a 442 kinase panel. There is a large drop off to cellular activity in both antiproliferative and biomarker assays and the contribution of each isoform to the response in the cellular environment is unknown. The cellular biomarker used, pS6RP, is indirect which should be considered when interpreting this data. PIM-447 shows a strong effect in a mouse xenograft study, with a pharmacodynamic response consistent with the in vitro data. Apart from the kinase selectivity and hERG activity, no broad pharmacological profiling data has been provided to further validate use of PIM-447 in vivo. Apr 10 2021 - 1:32pm
DESCRIPTION PIM447 is a potent and selective pan PIM kinase inhibitor , that is being investigated for clinical efficacy against hematological malignancies. (GtoPdb)
DESCRIPTION PIM447 (LGH447) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 displays dual antimyeloma and bone-protective effects. PIM447 induces apoptosis[1][2].
PRICE 433
DESCRIPTION PIM447 dihydrochloride (LGH447 dihydrochloride) is a potent, orally available, and selective pan-PIM kinase inhibitor, with Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively. PIM447 dihydrochloride displays dual antimyeloma and bone-protective effects. PIM447 dihydrochloride induces apoptosis[1][2].
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION PIM447 (LGH447) is an oral, selective pan-PIM kinase inhibitor with antitumor and bone-protective effects. It inhibits PIM1, PIM2, and PIM3, induces apoptosis, and decreases the viability, proliferation, and motility of HuH6 and COA67 cells. PIM447 suppresses tumorigenesis in hepatocellular carcinoma and can be used in the study of multiple myeloma. (TargetMol Bioactive Compound Library)
Cell lines
4
Organisms
0
Compound Sets
13
ChEMBL Drugs
CHEMBL3651966
Chemical Probes.org
pim-447
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB14943
DrugMAP
DMQN9ME
DMU26OE
EUbOPEN Chemogenomics Library
EUB0001581
Guide to Pharmacology
9790
High-quality chemical probes
PD076541
MedChem Express Bioactive Compound Library
HY-19322
HY-19322B
Novartis Chemogenetic Library (NIBR MoA Box)
Probe Miner (suitable probes)
P11309/474134
TargetMol Bioactive Compound Library
T12475
External IDs
24
Properties
(calculated by RDKit )
Molecular Weight
440.18
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
5.04
TPSA
80.9
Fraction CSP3
0.29
Chiral centers
3.0
Largest ring
6.0
QED
0.6
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Pim
Apoptosis
PIM1, PIM2, PIM3
Member status
virtual
MOA
Pim-1 Kinase Inhibitors
Pim-2 Kinase Inhibitors
Pim-3 Kinase Inhibitors
PIM kinase inhibitor
Target subclass
CAMK
CAMK, CAMK, CAMK
Target class
Protein kinase
Kinase, Kinase, Kinase
Orthogonal probe
SGI-1776,
Pathway
JAK/STAT Signaling
Chromatin/Epigenetic
Control
cpd 1
Recommended Cell Concentration
1 uM
Source data