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) ()
Cabozantinib hydrochloride ()
CabozantinibCT-XL184CometriqXL184C3627 ()
XL184 (S-malate) ()
BMS-907351 (S-malate) ()
BMS-907351 FREE BASE ()
CABOMETYX ()
COMETRIQ ()
XL-184 FREE BASE ()
Cabozantinib (BMS-907351) ()
Cabozantinib malate ()
XL184,BMS-907351 ()
Cabozantinib (s)-malate ()
P&D ID
PD003215
CAS
849217-68-1
1140909-48-3
1817759-42-4
Tags
available
drug
probe
Approved by
FDA
EMA
PMDA
First approval
2012
Drug indication
Ovarian cancer
non-small cell lung carcinoma
Neoplasm
Thyroid cancer
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe selectivity
protein-selective
Probe type
calculated probe
P&D approved
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Orthogonal probes
9
No orthogonal probes found
Similar probes
2
No structurally similar probes found
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)
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)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
44
Organisms
0
Compound Sets
38
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
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
Concise Guide to Pharmacology 2025/26
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
High-quality chemical probes
Informer Set
Kinase Inhibitors (best-in-class)
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Plus
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
461
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
Custom attributes
(extracted from source data)
Target
FLT3
KDR
MET
RET
VEGFR, MET, RET, KIT, FLT1, FLT3, FLT4, TIE2,AXL
VEGFR2
Apoptosis
AXL
c-Kit
c-Met
c-Met/HGFR
FLT4
TAM Receptor
VEGFR
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
RORα
RORγ
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

