General
Preferred name
naporafenib
Synonyms
LXH254 ()
N-{3-[2-(2-hydroxyethoxy)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-2-(trifluoromethyl)pyridine-4-carboxamide ()
Naporafenib (LXH254) ()
LXH 254 ()
LXH-254 ()
PAN-RAF INHIBITOR LXH254 ()
ERAS-254 ()
P&D ID
PD098291
CAS
1800398-38-2
Tags
available
drug candidate
Drug indication
Melanoma
Non-small-cell lung cancer
Drug Status
investigational
Max Phase
3.0
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 Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively[1][2].
PRICE 195
DESCRIPTION Naporafenib (LXH254) is an investigational, potent, selective and orally bioavailable RAF inhibitor that was designed to target RAS mutant cancers, i.e.those that harbour genetic alterations in the RAS-RAF-MEK-ERK (MAPK) pathway . It is one of the compounds claimed in Novartis' patent WO2014151616A1 . Naporafenib is a Type-2 kinase inhibitor that binds the DFG-out conformation of the kinase. (GtoPdb)
DESCRIPTION LXH254 is a pan-Raf inhibitor developed for the treatment of solid tumors. (BOC Sciences Bioactive Compounds)
DESCRIPTION LXH254 is a B/C RAF inhibitor with IC50 values of 0.2 nM and 0.07 nM for inhibiting BRAF and CRAF. (TargetMol Bioactive Compound Library)
Cell lines
3
Organisms
0
Compound Sets
13
AdooQ Bioactive Compound Library
A16841
BOC Sciences Bioactive Compounds
lxh254-cas-1800398-38-2-291271
Cayman Chemical Bioactives
28231
ChEMBL Drugs
CHEMBL4583691
Drug Repurposing Hub
DrugBank
DB18865
DrugMAP
DMQE9PS
Guide to Pharmacology
10658
MedChem Express Bioactive Compound Library
HY-112089
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
lxh254
TargetMol Bioactive Compound Library
T11898
External IDs
15
Properties
(calculated by RDKit )
Molecular Weight
502.18
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
3
cLogP
3.93
TPSA
96.81
Fraction CSP3
0.32
Chiral centers
0.0
Largest ring
6.0
QED
0.51
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
b-RAF
c-Raf
Raf
Bcr-Abl
p38 MAPK
MOA
Raf inhibitor
Pathway
MAPK/ERK Pathway
Protein Tyrosine Kinase/RTK
MAPK
Source data