General
Preferred name
tipifarnib
Synonyms
tipifarnib-P2 ()
R115777 ()
Zarnestra ()
IND 58359 ()
Tipifarnib (Zarnestra) ()
Tipifarnib (R115777) ()
Tipifarnib ()
R-11577 ()
R-115777 ()
NSC-702818 ()
P&D ID
PD003389
CAS
192185-72-1
192185-68-5
Tags
available
probe
drug candidate
Drug indication
Acute myeloid leukaemia
Myelodysplastic syndrome
Chronic lymphocytic leukemia
Chronic myelogenous leukaemia
Peripheral T-cell lymphoma
Colorectal cancer
Pancreatic cancer
Human papillomavirus infection
Drug Status
investigational
Max Phase
3.0
Probe info
Probe type
calculated probe
Probe selectivity
protein-selective
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
29
No orthogonal probes found
Similar probes
2
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
Tipifarnib is a non-peptidomimetic competitive farnesyltransferase inhibitor (FTI) .
(GtoPdb)
DESCRIPTION
Tipifarnib (IND 58359)?binds to and inhibits farnesyltransferase (FTase) with an IC50 of 0.86 nM. Antineoplastic activity and antiparasitic activity[1].
PRICE
130
DESCRIPTION
inhibitor of farnesyltransferase
(Informer Set)
DESCRIPTION
Potent and selective irreversible human rhinovirus 3C protease inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Tipifarnib is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Tipifarnib (IND 58359) is a nonpeptidomimetic quinolinone with potential antineoplastic activity. Tipifarnib binds to and inhibits the enzyme farnesyl protein transferase, an enzyme involved in protein processing (farnesylation) for signal transduction. By inhibiting the farnesylation of proteins, this agent prevents the activation of Ras oncogenes, inhibits cell growth, induces apoptosis, and inhibits angiogenesis.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
559
Organisms
1
Compound Sets
20
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
Pandemic Response Box
Probe Miner (suitable probes)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
37
Molecular Weight
488.12
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
5
Aromatic Ring Count
5
cLogP
5.5
TPSA
65.84
Fraction CSP3
0.11
Chiral centers
1.0
Largest ring
6.0
QED
0.36
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
FNTA
Farnesyl-transferase (FNTA)
Farnesyl Transferase
FNTA, FNTB
FTase,Transferase
Compound status
probe
Primary Target
Protein Prenyltransferases
MOA
Inhibitor
Inhibitors of Signal Transduction Pathways
Farnesyltransferase (geranylgeranyl pyrophosphate synthase) Inhibitors
farnesyltransferase inhibitor
Member status
member
Pathway
Metabolism
Metabolic Enzyme/Protease
Therapeutic Class
Anticancer Agents
Source data
