General
Preferred name
KRN 633
Synonyms
KRN-633 ()
KRN633 ()
VEGF receptor tyrosine kinase inhibitor III ()
K00589A ()
P&D ID
PD010972
CAS
286370-15-8
Tags
available
drug candidate
Drug indication
Glioma
Solid tumour/cancer
Drug Status
investigational
Max Phase
1.0
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
KRN633 is a potent and selective VEGFR inhibitor. which inhibits tyrosine phosphorylation of VEGFR-2 (IC50 = 1.16 nmol/L) in human umbilical vein endothelial cells. Selectivity profiling with recombinant tyrosine kinases showed that KRN633 is highly selective for VEGFR-1, -2, and -3. KRN633 inhibits tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. KRN633 also causes the regression of some well-established tumors and those that had regrown after the cessation of treatment. KRN633 was well tolerated and had no significant effects on body weight or the general health of the animals. KRN633 might be useful in the treatment of solid tumors and other diseases that depend on pathologic angiogenesis.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
16
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugMAP
Guide to Pharmacology
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
22
Molecular Weight
416.13
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
3
Aromatic Ring Count
3
cLogP
4.62
TPSA
94.6
Fraction CSP3
0.25
Chiral centers
0.0
Largest ring
6.0
QED
0.58
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Tyrosine Kinase/Adaptors
Angiogenesis
Protein Tyrosine Kinase/RTK
Target
VEGFR1
VEGFR2
VEGFR3
FLT1, FLT4, KDR
VEGFR
Member status
member
MOA
"Angiogenesis Inhibitors
Inhibitors of Signal Transduction Pathways
VEGFR-2 (FLK-1/KDR) Inhibitors"
Angiogenesis Inhibitors
VEGFR-2 (FLK-1/KDR) Inhibitors
VEGFR inhibitor
Therapeutic Class
Anticancer Agents
Source data
