General
Preferred name
TASELISIB
Synonyms
GDC-0032 ()
RG-7604 ()
RG7604 ()
Taselisib (GDC 0032) ()
GDC 0032 ()
P&D ID
PD012669
CAS
1282512-48-4
Tags
available
drug candidate
Drug indication
Breast cancer
non-Hodgkins lymphoma
Solid tumour/cancer
Drug Status
investigational
Max Phase
3.0
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
Taselisib is a potent and orally bioavailable kinase inhibitor which inhibits the PI3Kα, γ and δ isoforms but not the β isoform. It is compound 11l in .
(GtoPdb)
DESCRIPTION
Taselisib (GDC-0032) is a potent PI3K inhibitor targets PIK3CA mutations, with Kis of 0.12 nM, 0.29 nM, 0.97 nM, and 9.1 nM for PI3K¦Ä, PI3K¦Á, PI3K¦Ã and PI3K¦Â, respectively.
PRICE
87
DESCRIPTION
Taselisib, also known as GDC0032 or RG7606, is a selective, potent, orally bioavailable inhibitor of PI3Ka with a Ki = 0.2nM, and with reduced inhibitory activity against PI3K. This selectivity profile, and excellent pharmacokinetic and pharmaceutical properties, allowed for greater efficacy in vivo at the maximum tolerated dose relative to a pan Class I PI3K inhibitor in PIK3CA mutant xenografts. Notably, GDC-0032 preferentially inhibited PIK3CA mutant cells relative to cells with wild-type PI3K. GDC-0032 potently inhibits signal transduction downstream of PI3K and induces apoptosis at low concentrations in breast cancer cell lines and xenograft models that harbor PIK3CA mutations.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Taselisib (GDC-0032) is an orally bioavailable inhibitor of the class I phosphatidylinositol 3-kinase (PI3K) alpha isoform (PIK3CA), with potential antineoplastic activity.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
20
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
27
Molecular Weight
460.23
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
1
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
4
cLogP
3.17
TPSA
118.67
Fraction CSP3
0.38
Chiral centers
0.0
Largest ring
7.0
QED
0.49
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
C2β
PI3K
PI3Kα
PI3Kβ
PI3Kγ
PI3Kδ
PIK3CA
PIK3CD
PIK3CG
MOA
PI3K inhibitor
Pathway
Metabolism
PI3K/Akt/mTOR signaling
PI3K/Akt/mTOR
Recommended Cell Concentration
100 nM
Source data
