General
Preferred name
REGORAFENIB
Synonyms
BAY 73-4506 monohydrate ()
Stivarga, BAY-73-4506, BAY-734506 monohydrate ()
BAY 73-4506 ()
Fluoro-Sorafenib ()
BAY73-4506 hydrochloride ()
Regorafenib (BAY 73-4506) ()
Regorafenib (monohydrate) ()
Regorafenib (Hydrochloride) ()
BAY 73-4506 (monohydrate) ()
BAY 73-4506 (hydrochloride) ()
Fluoro-Sorafenib, Resihance, Stivarga,BAY 73-4506 ()
Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate ()
Stivarga, BAY 73-4506 hydrochloride ()
Regorafenib (BAY-734506) Monohydrate ()
Regorafenib Hydrochloride ()
Regorafenib Monohydrate ()
RegorafenibBAY 73-4506A-1112 ()
BAY-73-4506 ()
BAY-734506 ()
REGORAFENIB ANHYDROUS ()
REGORAFENIB HYDRATE ()
STIVARGA ()
BAY-73-4506 MONOHYDRATE ()
BAY-734506 MONOHYDRATE ()
Regorafenib-13C-d3 ()
P&D ID
PD003518
CAS
755037-03-7
1019206-88-2
835621-07-3
2126178-55-8
Tags
available
probe
drug
Approved by
FDA
EMA
First approval
2012
Drug indication
Metastatic colorectal cancer
colorectal adenocarcinoma
Drug Status
approved
Max Phase
4.0
Probe info
Probe type
calculated probe
Probe sources
Probe Miner (suitable 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)
HALF-LIFE Regorafenib, 160 mg oral dose = 28 hours (14 - 58 hours); ; M2 metabolite, 160 mg oral dose = 25 hours (14-32 hours); ; M5 metabolite, 160 mg oral dose = 51 hours (32-72 hours);
ABSORPTION Cmax = 2.5 μg/mL;; Tmax = 4 hours; ; AUC = 70.4 μg*h/mL; ; Cmax, steady-state = 3.9 μg/mL;; AUC, steady-state = 58.3 μg*h/mL;; The mean relative bioavailability of tablets compared to an oral solution is 69% to 83%.
DESCRIPTION Regorafenib is an inhibitor of multiple membrane-bound and intracellular kinases. Although the drug is approved it must carry a Boxed Warning alerting patients and clinicians that severe and fatal liver toxicity was observed in some patients in regorafenib clinical studies. Regorafenib is a Type-2 kinase inhibitor. (GtoPdb)
DESCRIPTION Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFR¦Â, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity[1].
PRICE 45
DESCRIPTION Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFR??, exhibiting both antitumor and anti-angiogenic activity.
DESCRIPTION Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFR¦Â, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity[1].
PRICE 41
DESCRIPTION Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-??, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.
DESCRIPTION Regorafenib Hydrochloride (BAY 73-4506 hydrochloride) is a multi-target inhibitor for VEGFR1/2/3, PDGFR¦Â, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively[1].
PRICE 47
DESCRIPTION inhibitor of BRAF, RET, KIT, and VEGFR2 (Informer Set)
DESCRIPTION Regorafenib is indicated for the treatment of patients with metastatic colorectal cancer (CRC) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy. Regorafenib is also indicated for the treatment of patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) who have been previously treated with imatinib mesylate and sunitinib malate. (PKIDB)
DESCRIPTION Regorafenib is a kinase inhibitor used to treat patients with metastatic colorectal cancer, unresectable, locally advanced, or metastatic gastrointestinal stromal tumors, and hepatocellular carcinoma. (Enamine Bioactive Compounds)
DESCRIPTION Regorafenib (BAY 73-4506) is an orally active, multi-targeted receptor tyrosine kinase inhibitor that inhibits RET, C-RAF, VEGFR2, c-Kit, VEGFR1, and PDGFRβ, exhibiting both antitumor and anti-angiogenic activity. (TargetMol Bioactive Compound Library)
DESCRIPTION Regorafenib Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, KIT, RET, RAF-1, B-RAF and B-RAF(V600E) respectively. (TargetMol Bioactive Compound Library)
DESCRIPTION Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity (TargetMol Bioactive Compound Library)
Cell lines
19
Organisms
2
Compound Sets
34
AdooQ Bioactive Compound Library
A10250
Axon Medchem Screening Library
1678
Cayman Chemical Bioactives
18498
25486
ChEMBL Approved Drugs
CHEMBL1946170
ChEMBL Drugs
CHEMBL1946170
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5891
Concise Guide to Pharmacology 2019/20
5891
Concise Guide to Pharmacology 2021/22
5891
Concise Guide to Pharmacology 2023/24
5891
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB08896
DrugBank Approved Drugs
DB08896
DrugCentral
4654
DrugCentral Approved Drugs
4654
DrugMAP
DMHSY1I
DrugMAP Approved Drugs
DMHSY1I
Enamine Bioactive Compounds
EBC-11382
EU-OPENSCREEN Bioactive Compound Library
EOS101246
Guide to Pharmacology
5891
Informer Set
628613
JUMP-Target 1 Compound Set
11167602
LINCS compound set
10225-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1946170
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1946170
MedChem Express Bioactive Compound Library
HY-10331
HY-10331A
HY-13308
NCATS Inxight Approved Drugs
24T2A1DOYB
NIH Approved Oncology Drugs
440809220
PKIDB
Probe Miner (suitable probes)
P34913/519928
ReFrame library
Selleckchem Bioactive Compound Library
BAY-73-4506
regorafenib-monohydrate
regorafenib-hydrochloride
TargetMol Bioactive Compound Library
T1792
T1792L
T8402
External IDs
60
Properties
(calculated by RDKit )
Molecular Weight
482.08
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
3
Rotatable Bonds
5
Ring Count
3
Aromatic Ring Count
3
cLogP
5.69
TPSA
92.35
Fraction CSP3
0.1
Chiral centers
0.0
Largest ring
6.0
QED
0.41
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
BRAF
KDR
KIT
RET
ABL1, BRAF, DDR2, EPHA2, FGFR1, FGFR2, FLT1, FLT4, FRK, KDR, KIT, MAPK11, NTRK1, PDGFRA, PDGFRB, RAF1, RET, TEK
RTK inhibitor
DDR2
PDGFR
Autophagy,c-Kit,c-RET,PDGFR,Raf,VEGFR
c-Kit,c-RET,PDGFR,Raf,VEGFR
FLT1
FLT4
PDGFRA
PDGFRB
FGFR1
FGFR2
TEK
NTRK1
EPHA2
RAF1
MAPK11
FRK
ABL1
FGFR
Tie
b-RAF
B-Raf (V600E)
murine VEGFR2
murine VEGFR3
PDGFRβ
Raf-1
VEGFR1
VEGFR2
Compound status
FDA
Targets
KDR,RET,RAF1
Pathway
Angiogenesis
Apoptosis
Autophagy
MAPK
Tyrosine Kinase/Adaptors
MAPK/ERK Pathway
Protein Tyrosine Kinase/RTK
MOA
c-Kit
c-RET
Raf
VEGFR
FGFR inhibitor, KIT inhibitor, PDGFR tyrosine kinase receptor inhibitor, RAF inhibitor, RET tyrosine kinase inhibitor, VEGFR inhibitor
Indication
colorectal cancer, gastrointestinal stromal tumors (GIST)
Source data