General
Preferred name
CABOZANTINIB
Synonyms
XL 184 ()
XL-184 ()
BMS-907351, Cometriq, Cabozantinib S-Malate, XL-184 ()
BMS-907351 ()
XL184 ()
Cabozantinib hydrochloride (849217-68-1(free base)) ()
XL184 free base ()
CABOZANTINIB S-MALATE ()
Cabozantinib (S-malate) ()
XL184 (S-malate) ()
BMS-907351 (S-malate) ()
XL184,BMS-907351 ()
Cabozantinib (BMS-907351) ()
Cabozantinib malate ()
Cabozantinib hydrochloride ()
CabozantinibCT-XL184CometriqXL184C3627 ()
BMS-907351 FREE BASE ()
CABOMETYX ()
COMETRIQ ()
XL-184 FREE BASE ()
Cabozantinib (s)-malate ()
P&D ID
PD003215
CAS
849217-68-1
1140909-48-3
1817759-42-4
Tags
available
probe
drug
Approved by
FDA
PMDA
EMA
First approval
2012
Drug indication
Thyroid cancer
Ovarian cancer
Neoplasm
non-small cell lung carcinoma
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
protein-selective
Probe sources
Chemical Probes.org
High-quality chemical probes
Probe targets
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 Cabozantinib is a Type-1, oral, small-molecule tyrosine kinase inhibitor.
Marketed formulations contain cabozantinib S-malate (PubChem CID 25102846). (GtoPdb)
DESCRIPTION Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis[1][2].
PRICE 55
DESCRIPTION Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
PRICE 57
DESCRIPTION Cabozantinib S-malate (XL184) is the s-malate salt form of cabozantinib, an orally bioavailable, small molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.
PRICE 101
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION inhibitor of c-MET, VEGFR2/3, and RET (Informer Set)
DESCRIPTION For the treatment of metastatic medullary thyroid cancer and for the treatment of patients with advanced renal cell carcinoma (RCC) who have received prior anti-angiogenic therapy. (PKIDB)
DESCRIPTION Potent VEGFR inhibitor; also inhibits other RTKs (Tocriscreen Plus)
DESCRIPTION High affinity PDEdelta-KRas interaction inhibitor; binds to PDEdelta (Tocris Bioactive Compound Library)
DESCRIPTION Cabozantinib (XL184) is a multi-targeted tyrosine kinase receptor inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt3 (IC50=0.035/1.3/4.6/7/11.3 nM). Cabozantinib exhibits both antitumor and antiangiogenic activity. (TargetMol Bioactive Compound Library)
DESCRIPTION Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM). (TargetMol Bioactive Compound Library)
Cell lines
40
Organisms
0
Compound Sets
37
AdooQ Bioactive Compound Library
A10996
A11349
Axon Medchem Screening Library
1819
Cayman Chemical Bioactives
18464
ChEMBL Approved Drugs
CHEMBL2105717
CHEMBL2103868
ChEMBL Drugs
CHEMBL2105717
CHEMBL2103868
Chemical Probes.org
cabozantinib
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5887
Concise Guide to Pharmacology 2019/20
5887
Concise Guide to Pharmacology 2021/22
5887
Concise Guide to Pharmacology 2023/24
5887
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08875
DrugBank Approved Drugs
DB08875
DrugCentral
4715
DrugCentral Approved Drugs
4715
DrugMAP
DMIYDT4
DrugMAP Approved Drugs
DMIYDT4
EU-OPENSCREEN Bioactive Compound Library
EOS101050
Guide to Pharmacology
5887
High-quality chemical probes
PD003215
Informer Set
660840
Kinase Inhibitors (best-in-class)
LINCS compound set
10194-106
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL2105717
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL2105717
MedChem Express Bioactive Compound Library
HY-13016
HY-12044
NCATS Inxight Approved Drugs
1C39JW444G
NIH Approved Oncology Drugs
440814386
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
XL184
cabozantinib-malate
TargetMol Bioactive Compound Library
T2586
T5164
Tocris Bioactive Compound Library
5422
Tocriscreen Plus
5422
Welcome Trust Cancer Drugs
249
External IDs
57
Properties
(calculated by RDKit )
Molecular Weight
501.17
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
8
Ring Count
5
Aromatic Ring Count
4
cLogP
5.54
TPSA
98.78
Fraction CSP3
0.18
Chiral centers
0.0
Largest ring
6.0
QED
0.31
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
FLT3
KDR
MET
RET
Apoptosis
VEGFR
VEGFR, MET, RET, KIT, FLT1, FLT3, FLT4, TIE2,AXL
VEGFR2
AXL
c-Kit
c-Met
c-Met/HGFR
FLT4
TAM Receptor
VEGFR2/KDR
KDR, MET, RET
MET/VEGFR2 inhibitor
Apoptosis related,Axl,c-Met,VEGFR
Apoptosis related,Axl,c-Kit,c-Met,c-RET,FLT3,VEGFR
RORĪ±
RORĪ³
Compound status
FDA
Target Type
Enzyme-Linked Receptors
Pathway
RTK signaling
Angiogenesis
Metabolism
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Known off targets
c-MET, RET, FLT1/3/4, Tie2, AXL
Kinase group
TK
MOA
Inhibitor
RET tyrosine kinase inhibitor, VEGFR inhibitor
Indication
medullary thyroid cancer (MTC)
Orthogonal probe
Brivanib
Target class
Protein kinase
Kinase
Source data