General
Preferred name
Poziotinib
Synonyms
HM-781-36B, NOV-120101 ()
HM781-36B ()
NOV120101 ()
HM 781-36B hydrochloride ()
NOV120101 hydrochloride ()
HM-78136B ()
Poziotinib (HM781-36B) ()
POZIOTINIB HYDROCHLORIDE ()
HM 781-36 ()
HM 781-36B ()
HM-781-36 ()
HM-781-36B ()
NOV-1201 ()
NOV-120101 ()
HM-781-36B hydrochloride ()
HM781-36B HYDROCHLORIDE ()
P&D ID
PD012535
CAS
1092364-38-9
1429757-68-5
Tags
available
covalent binder
drug candidate
Drug indication
Solid tumour/cancer
Non-small-cell lung cancer
HER2-positive breast cancer
Neoplasm
Drug Status
investigational
Max Phase
3.0
1.0
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 Poziotinib is an orally bioavailable, clinically active, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with antineoplastic activity . It is a potent inhibitor of the most common EGFR and HER2 exon 20 insertion mutants that are predominantly activating in nature, and resistant to exisitng reversible and irreversible EGFR tyrosine kinase inhibitors . (GtoPdb)
DESCRIPTION Poziotinib (HM781-36B) is an orally active, irreversible pan-HER inhibitor, which effectively inhibits EGFRwt, HER-2 and HER-4 with IC50s of 3.2, 5.3 and 23.5 nM, respectively. Poziotinib (HM781-36B) also shows excellent inhibitory activities against mutated EGFRs, including EGFRT790M and EGFRL858R/T790M, with IC50s of 4.2 and 2.2 nM, respectively. Excellent antitumor activity[1][2].
PRICE 96
PRICE 76
DESCRIPTION Poziotinib, also known as HM781-36B and NOV120101, is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity. HM781-36B irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. EGFRs, cell surface receptor tyrosine kinases, are often upregulated in a variety of cancer cell types and play key roles in cellular proliferation and survival. (BOC Sciences Bioactive Compounds)
DESCRIPTION Poziotinib (NOV120101)(NOV120101; HM781-36B) is an irreversible HER1/2/4 inhibitor (IC50s: 3/5/23 nM). (TargetMol Bioactive Compound Library)
DESCRIPTION Poziotinib hydrochloride irreversibly inhibits EGFR (HER1 or ErbB1), including EGFR mutants, HER2, and HER4, thereby inhibiting the proliferation of tumor cells that overexpress these receptors. It is an orally bioavailable, quinazoline-based pan epidermal growth factor receptor (EGFR or HER) inhibitor with potential antineoplastic activity. (TargetMol Bioactive Compound Library)
Cell lines
8
Organisms
0
Compound Sets
23
AdooQ Bioactive Compound Library
A13044
Axon Medchem Screening Library
2920
BOC Sciences Bioactive Compounds
poziotinib-cas-1092364-38-9-item-84-462151
Cayman Chemical Bioactives
22437
ChEMBL Drugs
CHEMBL3545154
CHEMBL5095402
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
7903
Concise Guide to Pharmacology 2019/20
7903
Concise Guide to Pharmacology 2021/22
7903
Concise Guide to Pharmacology 2023/24
7903
CovalentInDB
CI004909
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB12114
DrugMAP
DMZ3BER
EU-OPENSCREEN Bioactive Compound Library
EOS101609
Guide to Pharmacology
7903
LINCS compound set
10397-101
MedChem Express Bioactive Compound Library
HY-15730
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
poziotinib-hm781-36b
TargetMol Bioactive Compound Library
T2630
T8758
External IDs
38
Properties
(calculated by RDKit )
Molecular Weight
490.1
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
5.38
TPSA
76.58
Fraction CSP3
0.26
Chiral centers
0.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
EGFR,ERBB2,ERBB4
Target
Apoptosis
EGFR
HER1
HER2
HER4
EGFR, ERBB2, ERBB4
HER inhibitor
Apoptosis related,EGFR,HER2
MOA
EGFR inhibitor
Pathway
Angiogenesis
JAK/STAT Signaling
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Source data