General
Preferred name
APITOLISIB
Synonyms
RG-7422, G-038390, GDC-0980.1, G-038390.1, GDC-0980 ()
RG 7422 ()
GNE 390 ()
GDC-0980 ()
GDC-0980 (RG7422) ()
GDC 0980 ()
GDC-0980/RG7422 ()
G-038390 ()
G-038390.1 ()
GDC-0980.1 ()
GNE-390 ()
RG-7422 ()
RG7422 ()
Apitolisib (GDC-0980) ()
RG7422, GNE 390 ()
P&D ID
PD010882
CAS
1032754-93-0
Tags
available
probe
drug candidate
Drug indication
Solid tumour/cancer
Non-hodgkin lymphoma
non-Hodgkins lymphoma
Drug Status
investigational
Max Phase
2.0
Probe info
Probe type
P&D approved
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)
DESCRIPTION Apitolisib is a dual PI3K/mTOR inhibitor. Its discovery is described in , where it is compound 2 (GDC-0980). (GtoPdb)
DESCRIPTION Apitolisib (GDC-0980; GNE 390; RG 7422) is a selective, potent, orally bioavailable Class I PI3 kinase and mTOR kinase (TORC1/2) inhibitor with IC50s of 5 nM/27 nM/7 nM/14 nM for PI3K¦Á/PI3K¦Â/PI3K¦Ä/PI3K¦Ã, and with a Ki of 17 nM for mTOR.
PRICE 87
DESCRIPTION Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3K??(IC50=5 nM), PI3K??(IC50=27 nM), PI3K??(IC50=7 nM), PI3K?? (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others.
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION Apitolisib, also known as GDC-0980 and RG7422; or GNE390, is a dual PI3 kinase/mTOR inhibitor, is also an orally available agent targeting phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinase in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. PI3K/mTOR kinase inhibitor GDC-0980 inhibits both PI3K kinase and mTOR kinase, which may result in tumor cell apoptosis and growth inhibition of cancer cells overexpressing PI3K/mTOR. Activation of the PI3K/mTOR pathway promotes cell growth, survival, and resistance to chemotherapy and radiotherapy; mTOR, a serine/threonine kinase downstream of PI3K, may also be activated in a PI3K-independent fashion. (BOC Sciences Bioactive Compounds)
DESCRIPTION Apitolisib (RG 7422), an effective, class I PI3K inhibitor for PI3Kα(IC50=5 nM), PI3Kβ(IC50=27 nM), PI3Kδ(IC50=7 nM), PI3Kγ (IC50=14 nM), is used in trials study of solid cancers, breast cancer, prostate cancer, renal cell carcinoma, and endometrial carcinoma, among others. (TargetMol Bioactive Compound Library)
Cell lines
7
Organisms
1
Compound Sets
26
AdooQ Bioactive Compound Library
A11023
Axon Medchem Screening Library
1782
BOC Sciences Bioactive Compounds
apitolisib-cas-1032754-93-0-item-84-454921
Cayman Chemical Bioactives
18303
ChEMBL Drugs
CHEMBL1922094
Chemical Probes.org
gdc-0980
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
7888
Concise Guide to Pharmacology 2019/20
7888
Concise Guide to Pharmacology 2021/22
7888
Concise Guide to Pharmacology 2023/24
7888
Concise Guide to Pharmacology 2025/26
7888
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB12180
DrugMAP
DMF3MV1
EU-OPENSCREEN Bioactive Compound Library
EOS101306
Guide to Pharmacology
7888
High-quality chemical probes
PD010882
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1922094
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1922094
MedChem Express Bioactive Compound Library
HY-13246
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
GDC-0980-RG7422
TargetMol Bioactive Compound Library
T1916
External IDs
74
Properties
(calculated by RDKit )
Molecular Weight
498.22
Hydrogen Bond Acceptors
11
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
3
cLogP
0.9
TPSA
133.83
Fraction CSP3
0.52
Chiral centers
1.0
Largest ring
6.0
QED
0.52
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
PIK3CA,PIK3CB,PIK3CD,PIK3CG,MTOR
Target
FGR, MAP3K9, MTOR, PIK3CA, PIK3CB, PIK3CD, PIK3CG, SYK
PI3K/mTOR inhibitor
PIK3CA
MTOR
Apoptosis related,Autophagy,mTOR,PI3K
PI3K
p110α
p110β
p110γ
p110δ
PIK3CA, PIK3CB, PIK3CG, PIK3CD, MTOR
MOA
mTOR inhibitor, PI3K inhibitor
Pathway
Apoptosis
PI3K/Akt/mTOR signaling
PI3K/Akt/mTOR
Target class
Kinase, Kinase, Kinase, Kinase, Kinase
Target subclass
PI3/PI4, PI3/PI4, PI3/PI4, PI3/PI4, PI3/PI4
Source data