General
Preferred name
RAF-265
Synonyms
RAF265 ()
CHIR-265 ()
CHIR-265, NVP-RAF265 ()
RAF 265 ()
RAF265 (CHIR-265) ()
NVP-RAF265 ()
Raf 265 ()
P&D ID
PD003613
CAS
927880-90-8
Tags
available
drug candidate
Drug indication
Melanoma
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
CHIR-265 is an orally bioavailable inhibitor of RAF kinases, including the BRAF V600E mutant. It also inhibits phosphorylation of VEGFR2 (link to this abstract at AACR Meeting Abstracts Online #4876).
(GtoPdb)
DESCRIPTION
ihibitor of VEGFR2 and BRAF
(Informer Set)
DESCRIPTION
Potent and selective inhibitor of TGF-betaRI
(Tocris Bioactive Compound Library)
DESCRIPTION
RAF265 is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
3
Organisms
1
Compound Sets
23
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
31
Molecular Weight
518.13
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
5
cLogP
6.93
TPSA
80.65
Fraction CSP3
0.12
Chiral centers
0.0
Largest ring
6.0
QED
0.25
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
BRAF
KDR
b-RAF
VEGFR2
Raf
VEGFR
Apoptosis related,Raf,VEGFR
Compound status
clinical
Targets
CRAF,BRAF,KDR
Pathway
Angiogenesis
MAPK
Tyrosine Kinase/Adaptors
Apoptosis
Autophagy
MAPK/ERK Pathway
Protein Tyrosine Kinase/RTK
Primary Target
Raf Kinases
MOA
Inhibitor
RAF inhibitor, VEGFR inhibitor
Source data