General
Preferred name
FTI 276
Synonyms
FTI 276 (TFA) ()
FTI 276 trifluoroacetate salt ()
FTI-276 ()
FTI-276 (trifluoroacetate salt) ()
P&D ID
PD051053
CAS
1217471-51-6
170006-72-1
Tags
available
drug candidate
Drug indication
Discovery agent
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 This is the parent molecule of the ester prodrug FTI-277, which is the trifluoroacetate salt (PubChem CID 395753). The ester is designed to overcome the potential for thiol-based toxicity. FTI-276 is a peptidomimetic developed as a farnesyltransferase inhibitor (FTI) . (GtoPdb)
DESCRIPTION FTI-276 is a protein farnesyl transferase (PFT) inhibitor with IC50s of 0.9 nM and 0.5 nM for Plasmodium falciparum and human, respectively[1].
DESCRIPTION FTI-276 is a potent and selective farnesyltransferase inhibitor, which is also a tetrapeptide mimetic of the carboxyl terminus of K-Ras4B. FTI-276 blocked the growth in nude mice of a human lung carcinoma that expresses the two most prevalent genetic alterations in human cancers (K-Ras oncogenic mutation and deletion in the tumor suppressor gene p53). In contrast, FTI-276 did not inhibit tumor growth of a human lung carcinoma that harbors no Ras mutations. Furthermore, FTI-276 inhibited oncogenic signaling and tumor growth of NIH 3T3 cells transformed with the ras but not the raf oncogene. (BOC Sciences Bioactive Compounds)
DESCRIPTION FTI 276 is a Ras CAAX peptidomimetic, a selective inhibitor of farnesyltransferase (FTase) with > 100-fold selectivity over geranylgeranyltransferase I (GGTase I) (IC50 = 0.5 and 50 nM, respectively). It exhibits an inhibitory effect on growth of human lung carcinoma expressing oncogenic K-Ras in nude mice. (BOC Sciences Bioactive Compounds)
Cell lines
2
Organisms
0
Compound Sets
6
BOC Sciences Bioactive Compounds
fti-276-cas-170006-72-1-item-84-272116
fti-276-trifluoroacetate-salt-cas-1217471-51-6-item-119108
Cayman Chemical Bioactives
10011661
DrugMAP
DMN2Q7Y
Guide to Pharmacology
6531
MedChem Express Bioactive Compound Library
HY-15873A
Novartis Chemogenetic Library (NIBR MoA Box)
External IDs
27
Properties
(calculated by RDKit )
Molecular Weight
433.15
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
5
Rotatable Bonds
11
Ring Count
2
Aromatic Ring Count
2
cLogP
2.96
TPSA
104.45
Fraction CSP3
0.33
Chiral centers
2.0
Largest ring
6.0
QED
0.35
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Farnesyl Transferase
Pathway
Metabolic Enzyme/Protease
Member status
virtual
MOA
Farnesyltransferase (geranylgeranyl pyrophosphate synthase) Inhibitors
Inhibitors of Signal Transduction Pathways
Source data