U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C24H25N5O4
Molecular Weight 447.4864
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AZD-2932

SMILES

COC1=CC2=NC=NC(OC3=CC=C(CC(=O)NC4=CN(N=C4)C(C)C)C=C3)=C2C=C1OC

InChI

InChIKey=TWYCZJMOEMMCGC-UHFFFAOYSA-N
InChI=1S/C24H25N5O4/c1-15(2)29-13-17(12-27-29)28-23(30)9-16-5-7-18(8-6-16)33-24-19-10-21(31-3)22(32-4)11-20(19)25-14-26-24/h5-8,10-15H,9H2,1-4H3,(H,28,30)

HIDE SMILES / InChI

Molecular Formula C24H25N5O4
Molecular Weight 447.4864
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

AZD2932 is an oral inhibitor of VEGFR-2 and PDGFR tyrosine kinases, which was developed by AstraZeneca as a potential anti-cancer medicine. The drug was tested in vivo in preclinical model of mice bearing C6 rat glial tumors and AZD2932 demonstrated good potency: growth of Calu-6 tumor was inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. and LoVo tumors by 67% at 50 mg/kg b.i.d.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: P35968
Gene ID: 3791.0
Gene Symbol: KDR
Target Organism: Homo sapiens (Human)
8.0 nM [IC50]
Target ID: P09619
Gene ID: 5159.0
Gene Symbol: PDGFRB
Target Organism: Homo sapiens (Human)
4.0 nM [IC50]
Target ID: P16234
Gene ID: 5156.0
Gene Symbol: PDGFRA
Target Organism: Homo sapiens (Human)
2.0 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
PubMed

PubMed

TitleDatePubMed
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.
2012 Jan 1
Patents

Sample Use Guides

Preclinical model: AZD2932 is given orally twice a day at a dose 12.5 or 50 mg/kg.
Route of Administration: Oral
In Vitro Use Guide
Unknown
Substance Class Chemical
Created
by admin
on Sat Dec 16 12:11:18 UTC 2023
Edited
by admin
on Sat Dec 16 12:11:18 UTC 2023
Record UNII
SJ9PP5S9IM
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AZD-2932
Code English
4-((6,7-DIMETHOXY-4-QUINAZOLINYL)OXY)-N-(1-(1-METHYLETHYL)-1H-PYRAZOL-4-YL)BENZENEACETAMIDE
Systematic Name English
BENZENEACETAMIDE, 4-((6,7-DIMETHOXY-4-QUINAZOLINYL)OXY)-N-(1-(1-METHYLETHYL)-1H-PYRAZOL-4-YL)-
Systematic Name English
Code System Code Type Description
CAS
883986-34-3
Created by admin on Sat Dec 16 12:11:18 UTC 2023 , Edited by admin on Sat Dec 16 12:11:18 UTC 2023
PRIMARY
PUBCHEM
11517980
Created by admin on Sat Dec 16 12:11:18 UTC 2023 , Edited by admin on Sat Dec 16 12:11:18 UTC 2023
PRIMARY
FDA UNII
SJ9PP5S9IM
Created by admin on Sat Dec 16 12:11:18 UTC 2023 , Edited by admin on Sat Dec 16 12:11:18 UTC 2023
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
COMPETITIVE INHIBITOR
IC50
Related Record Type Details
ACTIVE MOIETY