General
Preferred name
TOCERANIB
Synonyms
PHA 291639 (phosphate) ()
PHA 291639 ()
PHA 291639E ()
SU11654 ()
SU11654 phosphate ()
PHA 291639 phosphate ()
Toceranib (phosphate) ()
SU11654 (phosphate) ()
PHA 291639E (phosphate) ()
Palladia, SU11654 ()
TOCERANIB PHOSPHATE ()
PALLADIA ()
PHA-291639 ()
PHA-291639E ()
P&D ID
PD012957
CAS
356068-94-5
874819-74-6
Tags
available
drug candidate
Approved by
FDA
Drug Status
vet_approved
investigational
Max Phase
2.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PRICE 1300
DESCRIPTION Toceranib (PHA-291639 and formerly SU11654) is a small molecule, multi-targeted receptor tyrosine kinase inhibitor . It is structurally related to . Targets include VEGFRs, FGFR, PDGFRs, and Kit (including constitutively active mutant forms ). Like sunitinib, toceranib has antiangiogenic and anitproliferative actions. Palladiar® branded toceranib is used to treat solid tumours in dogs. (GtoPdb)
PRICE 32
DESCRIPTION Toceranib (PHA 291639E) phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFR?? and Flk-1/KDR, respectively), has antitumor and antiangiogenic activity.
DESCRIPTION Toceranib Phosphate (SU11654 phosphate), is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR (TargetMol Bioactive Compound Library)
DESCRIPTION Toceranib (CAS 356068-94-5) is a potent ATP-competitive PDGFR and VEGFR inhibitor (Ki = 5 and 6 nM, respectively); inhibits phosphorylation of c-Kit and suppresses the growth of mast cell lines expressing mutant Kit, inducing cell cycle arrest and apoptosis. Also inhibits FGFR1 (Ki = 0.5 μM). Effective in vivo. (BOC Sciences Bioactive Compounds)
DESCRIPTION Toceranib is an orally active receptor tyrosine kinase inhibitor, and it potently inhibits PDGFR, VEGFR, and Kit. (Enamine Bioactive Compounds)
DESCRIPTION Toceranib (PHA 291639E) phosphate is an orally active inhibitor of tyrosine kinase (RTK) receptor, and it potently inhibits PDGFR, VEGFR, and Kit(with Kis of 5 and 6 nM for PDGFRβ and Flk-1/KDR, respectively), has antitumor and antiangiogenic activity. (TargetMol Bioactive Compound Library)
Compound Sets
12
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
Drug Repurposing Hub
DrugCentral
Enamine Bioactive Compounds
Guide to Pharmacology
MedChem Express Bioactive Compound Library
PKIDB
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
External IDs
33
Properties
(calculated by RDKit )
Molecular Weight
396.2
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
3
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
2
cLogP
3.09
TPSA
77.23
Fraction CSP3
0.36
Chiral centers
0.0
Largest ring
6.0
QED
0.68
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
c-Kit
KIT
PDGFR
VEGFR
tyrosine kinase
PDGFR??
FLT1, FLT3, KDR, PDGFRA, PDGFRB
PDGFR,VEGFR
Indication
cutaneous mast cell tumors
MOA
protein tyrosine kinase inhibitor
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Proteases/Proteasome
Protein Tyrosine Kinase/RTK
Source data