General
Preferred name
SAR-260301
Synonyms
compound 28 [PMID: 24387221] ()
SAR260301 ()
SAR260301 ()
P&D ID
PD049835
CAS
1260612-13-2
Tags
available
drug candidate
Drug Status
investigational
Max Phase
1.0
Drug indication
Neoplasm
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 Compound 28 is reported in a discovery effort to optimize pyrimidone indoline amide inhibitors of PI3Kβ .
DESCRIPTION SAR-260301 is an orally available and selective PI3K¦Â inhibitor with an IC50 of 23 nM[1][2].
PRICE 75
DESCRIPTION SAR-260301, an orally available and selective inhibitor of PI3K?? [IC50: 23 nM].
DESCRIPTION SAR260301 (compound 28 [PMID: 24387221]) was reported in a discovery effort to optimize pyrimidone indoline amide inhibitors of PI3Kβ . It is an orally bioavailable compound that is selective for PI3Kβ over other PI3 kinases. (GtoPdb)
DESCRIPTION SAR260301 is potent and selective Class I phosphatidylinositol-3-kinase (PI3K)β specific inhibitor with an IC50 of 52 nM for this isoform. SAR260301 is being investigated for the treatment of PTEN-deficient tumors. SAR260301 displayed improved physicochemical and in vitro pharmacokinetic properties. SAR260301 demonstrated significant in vivo activity in a UACC-62 xenograft model in mice, warranting further preclinical investigation. (BOC Sciences Bioactive Compounds)
Cell lines
0
Organisms
1
Compound Sets
7
BOC Sciences Bioactive Compounds
sar260301-cas-1260612-13-2-item-84-462781
Cayman Chemical Bioactives
17391
ChEMBL Drugs
CHEMBL3112866
EU-OPENSCREEN Bioactive Compound Library
EOS101272
Guide to Pharmacology
8793
MedChem Express Bioactive Compound Library
HY-15837
ReFrame library
External IDs
18
Properties
(calculated by RDKit )
Molecular Weight
354.17
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
4
Aromatic Ring Count
2
cLogP
1.13
TPSA
78.53
Fraction CSP3
0.42
Chiral centers
1.0
Largest ring
6.0
QED
0.89
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
PI3K
Pathway
PI3K/Akt/mTOR
Source data