General
Preferred name
linsitinib
Synonyms
OSI-906, ASP-7487, OSI-906AA ()
OSI-906 ()
OSI 906 ()
OSI906 ()
ASP-7487 ()
OSI-906AA ()
Linsitinib (OSI-906) ()
P&D ID
PD011146
CAS
867160-71-2
1356958-77-4
Tags
available
probe
drug candidate
Drug Status
investigational
Max Phase
3.0
Probe info
Probe type
experimental probe
Probe sources
Chemical Probes.org
High-quality chemical 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 This is the best available probe for INSRR and IRR. A panel of 88 kinases was profiled when selectivity was assessed. Aug 3 2017 - 3:34pm; Linsitinib (OSI-906) has excellent kinase selectivity, and is quite potent against the indicated kinases that it does inhibit. It shows very good in vivo activity, and is orally bioavailable. Together, these properties make linsitinib a high-quality probe for INSR and IGF-1R activity in cells and in vivo. Nov 10 2020 - 12:16pm; This is a dual selective  IGF1R & INSR (and related INSRR) kinase inhibitor with demonstrated kinase selectivity an cell-based assay activity with oral bioavailability. Nov 16 2020 - 8:46pm
DESCRIPTION Note that the chemical structure in the PubChem record is for the non-stereo molecule. The INN record specifies stereochemistry as shown in our chemical structure. (GtoPdb)
MOA Inhibitor (Chemical Probes.org)
Cell lines
437
Organisms
1
Compound Sets
20
Axon Medchem Screening Library
1702
Cayman Chemical Bioactives
17708
ChEMBL Drugs
CHEMBL1091644
Chemical Probes.org
linsitinib
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DB06075
EU-OPENSCREEN Bioactive Compound Library
EOS100605
EUbOPEN Chemogenomics Library
EUB0000614
Guide to Pharmacology
7423
High-quality chemical probes
PD011146
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1091644
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1091644
MedChem Express Bioactive Compound Library
HY-10191
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
OSI-906
TargetMol Bioactive Compound Library
T6017
The Pathogen Box
External IDs
31
Properties
(calculated by RDKit )
Molecular Weight
421.19
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
3
Ring Count
6
Aromatic Ring Count
5
cLogP
4.82
TPSA
89.33
Fraction CSP3
0.19
Chiral centers
0.0
Largest ring
6.0
QED
0.44
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Disease
MALARIA
Targets
IGF1R
Pathway
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Target
IGF-1R
Insulin Receptor
IRR
IGF1R, INSR, INSRR
IGF1R inhibitor
Member status
member
MOA
IGF-1R Inhibitors
Insulin Receptor Antagonists
IGF-1 inhibitor
Target subclass
TK
TK, TK, TK
Target class
Protein kinase
Kinase, Kinase, Kinase
Recommended Cell Concentration
1 µM
Source data