General
Preferred name
CH-5132799
Synonyms
PA-799 ()
lzorlisib ()
CH5132799 ()
izorlisib ()
MEN1611, PA799 ()
CH 5132799 ()
PA799 ()
CH5132799-000 ()
P&D ID
PD010879
CAS
1007207-67-1
Tags
available
drug candidate
Drug indication
Colorectal cancer
Neoplasm
Solid tumour/cancer
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
CH5132799 is described as a potent, orally available class I PI3K inhibitor . Clinical development of CH5132799 is being licenced to Menarini Pharma from Chugai Pharmaceutical Co.
DESCRIPTION
Izorlisib (MEN1611 and formerly CH5132799) is described as a potent, orally available class I PI3K inhibitor . Clinical development of CH5132799 has been licenced to Menarini Pharma from Chugai Pharmaceutical Co, hence the change in research code.
The chemical structure of MEN1611 is identical to that which was submitted to the WHO for the INN izorlisib (proposed INN list 126, Jan 2022). (GtoPdb)
The chemical structure of MEN1611 is identical to that which was submitted to the WHO for the INN izorlisib (proposed INN list 126, Jan 2022). (GtoPdb)
DESCRIPTION
Izorlisib (CH5132799) is a selective class I PI3K inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3K¦Á, with an IC50 of 14 nM.
PRICE
193
DESCRIPTION
CH5132799 is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3K; (IC(50)=0.014 uM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
CH5132799 has been used in trials studying the treatment of Solid Tumors.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
5
Organisms
0
Compound Sets
15
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
24
Molecular Weight
377.13
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
4
Aromatic Ring Count
2
cLogP
-0.33
TPSA
127.43
Fraction CSP3
0.47
Chiral centers
0.0
Largest ring
6.0
QED
0.76
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Member status
member
MOA
Phosphatidylinositol 3-Kinase beta (PI3Kbeta) Inhibitors
Phosphatidylinositol 3-Kinase alpha (PI3Kalpha) Inhibitors
Phosphatidylinositol 3-Kinase gamma (PI3Kgamma) Inhibitors
PI3K inhibitor
Target
MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG
PI3K
MTOR
PI3Kα
PI3Kβ
PI3Kγ
PI3Kδ
Pathway
PI3K/Akt/mTOR signaling
PI3K/Akt/mTOR
Source data
