General
Preferred name
vactosertib
Synonyms
EW-7197 ()
TEW-7197 ()
EW-7197 Hydrochloride ()
NOV1301 Hydrochloride ()
NOV 1301 Hydrochloride ()
TEW-7197 Hydrochloride ()
Vactosertib (Hydrochloride) ()
EW-7197 (Hydrochloride) ()
TEW-7197 (Hydrochloride) ()
Vactosertib (TEW-7197) ()
Vactosertib Hydrochloride ()
TEW 7197 ()
P&D ID
PD021555
CAS
1352608-82-2
1352610-25-3
Tags
available
drug candidate
Drug indication
Myeloproliferative neoplasm
Urothelial carcinoma
Myelodysplastic syndrome
Solid tumour/cancer
Drug Status
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)
DESCRIPTION The discovery of EW-7197 is reported in where it is compound 12b. EW-7197 acts as in inhibitor of transforming growth factor beta receptor 1B (ALK5) and activin A receptor type IB (ALK4). The compound is potent, selective, and orally bioavailable.
DESCRIPTION The discovery of EW-7197 is reported in where it is compound 12b. EW-7197 acts as in inhibitor of transforming growth factor beta receptor 1B (ALK5) and activin A receptor type IB (ALK4). The compound is potent, selective, and orally bioavailable, and exhibits experimental anti-tumour activity. Proposed INN is vactosertib.
DESCRIPTION The discovery of vactosertib (EW-7197) is reported in where it is compound 12b. EW-7197 acts as in inhibitor of transforming growth factor beta receptor 1B (TGFβR1; ALK5) and activin A receptor type IB (ACVR1B; ALK4). The compound is potent, selective, and orally bioavailable, and exhibits experimental anti-tumour activity. (GtoPdb)
DESCRIPTION Vactosertib (EW-7197) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib has potently antimetastatic activity and anticancer effect[1][2].
PRICE 83
DESCRIPTION Vactosertib Hydrochloride (EW-7197 Hydrochloride) is a potent, orally active and ATP-competitive activin receptor-like kinase 5 (ALK5) inhibitor with an IC50 of 12.9 nM. Vactosertib Hydrochloride also inhibits ALK2 and ALK4 (IC50 of 17.3 nM) at nanomolar concentrations. Vactosertib Hydrochloride has potently antimetastatic activity and anticancer effect[1][2].
PRICE 90
DESCRIPTION Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally active and highly efficient ATP-competitive ALK5 (activin receptor-like kinase 5) inhibitor, a TGF-?? receptor I inhibitor with anti-metastatic and anticancer properties. It sensitizes pancreatic cancer cells to gemcitabine by inhibiting their viability.
DESCRIPTION Vactosertib (EW-7197) acts as in inhibitor of transforming growth factor beta receptor 1B (ALK5) and activin A receptor type IB (ALK4). The compound is potent, selective, and orally bioavailable, and exhibits experimental anti-tumour activity. (PKIDB)
DESCRIPTION Vactosertib (EW-7197) is an orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity. (TargetMol Bioactive Compound Library)
DESCRIPTION Vactosertib Hydrochloride (EW-7197 Hydrochloride) is an orally active and highly efficient ATP-competitive ALK5 (activin receptor-like kinase 5) inhibitor, a TGF-β receptor I inhibitor with anti-metastatic and anticancer properties. It sensitizes pancreatic cancer cells to gemcitabine by inhibiting their viability. (TargetMol Bioactive Compound Library)
Compound Sets
19
AdooQ Bioactive Compound Library
A14213
Cayman Chemical Bioactives
19231
ChEMBL Drugs
CHEMBL3260567
Concise Guide to Pharmacology 2017/18
8107
Concise Guide to Pharmacology 2019/20
8107
Concise Guide to Pharmacology 2021/22
8107
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB15310
DrugMAP
DM2LBC3
EU-OPENSCREEN Bioactive Compound Library
EOS101262
EUbOPEN Chemogenomics Library
EUB0000041
Guide to Pharmacology
8107
LINCS compound set
10447-101
MedChem Express Bioactive Compound Library
HY-19928
HY-19928A
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
ew-7197
TargetMol Bioactive Compound Library
T6496
T15262
External IDs
30
Properties
(calculated by RDKit )
Molecular Weight
399.16
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
5
Aromatic Ring Count
5
cLogP
4.24
TPSA
83.79
Fraction CSP3
0.09
Chiral centers
0.0
Largest ring
6.0
QED
0.46
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
TGF-¦Â Receptor
ALK5
TGF-??Receptor
ACVR1B, TGFBR1
TGF-β Receptor
ALK1
ALK2
ALK3
ALK4
Pathway
Angiogenesis
Stem Cells
Tyrosine Kinase/Adaptors
TGF-beta/Smad
MOA
TGF beta receptor inhibitor
Recommended Cell Concentration
100 nM
Source data