General
Preferred name
Bemcentinib
Synonyms
R428 ()
BGB324 ()
R 428 dihydrochloride ()
R-428 ()
Bemcentinib (R428) ()
BGB 324 ()
BGB-324 ()
CS-1046 ()
HY-15150 ()
KB-80319 ()
QC-11751 ()
R 428 ()
SYN-1131 ()
SYN1131 ()
W-5845 ()
R428 ()
P&D ID
PD003525
CAS
1037624-75-1
Tags
available
drug candidate
Drug indication
Non-small-cell lung cancer
Triple negative breast cancer
Myelodysplastic syndrome
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
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Bemcentinib (BGB324, R428) is a potent, selective and orally active AXL receptor tyrosine kinase inhibitor that was discovered by Rigel as R428 and which is being developed by BergenBio for anti-cancer potential .
(GtoPdb)
DESCRIPTION
Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer[1][2].
PRICE
147
DESCRIPTION
inhibitor of the tyrosine-protein kinase receptor UFO
(Informer Set)
DESCRIPTION
Bemcentinib (R428) is a selective inhibitor of Axl (IC50: 14 nM) and has been investigated for the treatment of NSCLC.
(TargetMol Bioactive Compound Library)
DESCRIPTION
R 428 dihydrochloride is a potent and selective inhibitor of Axl receptor tyrosine kinases (IC50 = 14 nM). R428 inhibits Axl kinase and Axl-dependent events, including Akt phosphorylation, breast cancer cell invasion, and proinflammatory cytokine production.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
3
Organisms
0
Compound Sets
18
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
Mcule NIBR MoA Box Subset
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
36
Molecular Weight
506.29
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
4
Ring Count
7
Aromatic Ring Count
4
cLogP
4.88
TPSA
97.78
Fraction CSP3
0.4
Chiral centers
1.0
Largest ring
7.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
AXL
TAM Receptor
Axl inhibitor
Compound status
probe
Member status
member
MOA
Axl tyrosine kinase receptor inhibitor
Axl kinase inhibitor
Pathway
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Source data
