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Details

Stereochemistry ACHIRAL
Molecular Formula C23H21Cl2FN4O3.ClH
Molecular Weight 527.8039
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of POZIOTINIB HYDROCHLORIDE

SMILES

C=CC(=O)N1CCC(CC1)Oc2cc3c(cc2OC)ncnc3Nc4ccc(c(c4F)Cl)Cl.Cl

InChI

InChIKey=OMYSOLOMWJFVNK-UHFFFAOYSA-N
InChI=1S/C23H21Cl2FN4O3.ClH/c1-3-20(31)30-8-6-13(7-9-30)33-19-10-14-17(11-18(19)32-2)27-12-28-23(14)29-16-5-4-15(24)21(25)22(16)26;/h3-5,10-13H,1,6-9H2,2H3,(H,27,28,29);1H

HIDE SMILES / InChI

Molecular Formula C23H21Cl2FN4O3
Molecular Weight 491.343
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Molecular Formula ClH
Molecular Weight 36.4609
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Poziotinib is an inhibitor of EGFR tyrosine kinase family. The drug is being tested in phase II of clinical trials for different cancers: breast cancer, lung adenocarcinoma, head and neck squamous cell carcinoma, HER-2 positive advanced gastric cancer (in combination with Paclitaxel and Trastuzumab).

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
3.2 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Antitumor activity of HM781-36B, a highly effective pan-HER inhibitor in erlotinib-resistant NSCLC and other EGFR-dependent cancer models.
2012 May 15
Patents

Sample Use Guides

Head and Neck Squamous Cell Carcinoma: Take 45 mg orally, daily and continuously. Lung Adenocarcinoma: patients should receive poziotinib at dose of 16 mg orally once daily in a 28-day cycle.
Route of Administration: Oral
HCC827 cells were inhibited on 50% at 1.2 nM of poziotinib; NCI-H358 cells - at 4.8 nM; NCI-H1975 cells - at 5.7 nM; Calu-3 cells - at 2.1 nM; NCI-H1781 cells - at 4 nM; SK-Br3 cells - at 1 nM; NCI-N87 cells - at 0.6 nM.
Substance Class Chemical
Created
by admin
on Sat Jun 26 06:32:54 UTC 2021
Edited
by admin
on Sat Jun 26 06:32:54 UTC 2021
Record UNII
X4Z7U6JL1C
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
POZIOTINIB HYDROCHLORIDE
Common Name English
HM781-36B
Code English
HM 781-36B
Code English
2-PROPEN-1-ONE, 1-(4-((4-((3,4-DICHLORO-2-FLUOROPHENYL)AMINO)-7-METHOXY-6-QUINAZOLINYL)OXY)-1-PIPERIDINYL)-, HYDROCHLORIDE (1:1)
Systematic Name English
1-(4-(4-(3,4-DICHLORO-2-FLUOROPHENYLAMINO)-7-METHOXYQUINAZOLIN-6-YLOXY)-PIPERIDIN-1-YL)PROP-2-EN-1-ONE HYDROCHLORIDE
Systematic Name English
HM-781-36B
Code English
Code System Code Type Description
FDA UNII
X4Z7U6JL1C
Created by admin on Sat Jun 26 06:32:54 UTC 2021 , Edited by admin on Sat Jun 26 06:32:54 UTC 2021
PRIMARY
PUBCHEM
54767257
Created by admin on Sat Jun 26 06:32:54 UTC 2021 , Edited by admin on Sat Jun 26 06:32:54 UTC 2021
PRIMARY
NCI_THESAURUS
C176878
Created by admin on Sat Jun 26 06:32:54 UTC 2021 , Edited by admin on Sat Jun 26 06:32:54 UTC 2021
PRIMARY
CAS
1429757-68-5
Created by admin on Sat Jun 26 06:32:54 UTC 2021 , Edited by admin on Sat Jun 26 06:32:54 UTC 2021
PRIMARY
Related Record Type Details
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