General
Preferred name
VARLITINIB
Synonyms
ARRY-543, ASLAN-001, AR-00334543, ARRY-334543, Varlitinib Tosylate ()
AR-00334543 ()
ARRY-334543 ()
ARRY-543 ()
ASLAN-001 ()
ASLAN001 ()
Varlitinib tosylate ()
ARRY334543 ()
AR00334543 ARRY-334543 ARRY-543 ()
Varlitinib tosilate ()
AR00334543 ()
Arry-334543 ditosilate ()
Ar00334543 ditosilate ()
Arry-543 ditosilate ()
P&D ID
PD010682
CAS
845272-21-1
Tags
available
drug candidate
Drug indication
Metastatic biliary tract neoplasms
Breast cancer
Drug Status
investigational
Max Phase
Phase 2
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 Varlitinib selectively and reversibly binds to both EGFR and HER2 and prevents their phosphorylation and activation, and is being investigated for the treatment of some types of cancer. Some bioactivity data may be linked to the tosylate salt (PubChem CID 56842258).
This clinical candidate has completed Phase II clinical trials. Click here to view varlitinib trials registered with ClinicalTrials.gov. (GtoPdb)
MOA Varlitinib is an orally active, reversible, enzymatic and cellular inhibitor, with nanomolar potency, of the key growth factor receptor tyrosine kinases ErbB-2 and EGFR. The compound possesses improved physiochemical properties relative to compounds directed at these targets currently in clinical development, and provides superior exposure and equivalent or greater efficacy in animal models of human cancer. Currently, there is no single drug on the market that selectively inhibits both ErbB-2 and EGFR. Varlitinib, which concurrently inhibits the molecular targets of the drugs Herceptin(R) (ErbB-2) and Erbitux(R) (EGFR), may provide enhanced efficacy in the treatment of cancer patients.;
DESCRIPTION Investigated for use/treatment in cancer/tumors (unspecified). (PKIDB)
DESCRIPTION Varlitinib, also known as ARRY-543, is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus). (last updated ). (BOC Sciences Bioactive Compounds)
Compound Sets
13
BOC Sciences Bioactive Compounds
varlitinib-cas-845272-21-1-item-84-459804
Cayman Chemical Bioactives
27651
ChEMBL Drugs
CHEMBL2103842
CHEMBL2105679
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DB05944
DrugMAP
DMDG8Q3
EU-OPENSCREEN Bioactive Compound Library
EOS100578
Guide to Pharmacology
7645
MedChem Express Bioactive Compound Library
HY-10530
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
arry334543
External IDs
32
Properties
(calculated by RDKit )
Molecular Weight
466.1
Hydrogen Bond Acceptors
9
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
5
Aromatic Ring Count
4
cLogP
5.25
TPSA
93.55
Fraction CSP3
0.18
Chiral centers
1.0
Largest ring
6.0
QED
0.4
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
EGFR,ERBB2
Target
ERBB2
EGFR
MOA
EGFR inhibitor
Pathway
JAK/STAT Signaling
Protein Tyrosine Kinase/RTK
Source data