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Details

Stereochemistry ABSOLUTE
Molecular Formula C22H24N4O4
Molecular Weight 408.4504
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of AZD-6482

SMILES

C[C@@H](NC1=C(C=CC=C1)C(O)=O)C2=CC(C)=CN3C(=O)C=C(N=C23)N4CCOCC4

InChI

InChIKey=IRTDIKMSKMREGO-OAHLLOKOSA-N
InChI=1S/C22H24N4O4/c1-14-11-17(15(2)23-18-6-4-3-5-16(18)22(28)29)21-24-19(12-20(27)26(21)13-14)25-7-9-30-10-8-25/h3-6,11-13,15,23H,7-10H2,1-2H3,(H,28,29)/t15-/m1/s1

HIDE SMILES / InChI

Molecular Formula C22H24N4O4
Molecular Weight 408.4504
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/25042253

AZD-6482 is being developed by AstraZeneca to evaluate its therapeutic effects in the treatment of thrombosis. AZD-6482 is essentially a PI3K-beta inhibitor. It is a PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ in cell-free assays. by targeting PI3Kβ, AZD-6482 specifically inhibits thrombosis without interfering with normal haemostasis. Therefore, AZD-6482 is used as an anti-thrombotic drug for the prophylaxis of thrombotic disorders. AZD-6482 was in phase I trials by AstraZeneca for the prevention of thrombosis. However, the study was discontinued.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: O00459
Gene ID: 5296.0
Gene Symbol: PIK3R2
Target Organism: Homo sapiens (Human)
10.0 nM [IC50]
0.27 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Preventing
Unknown

Approved Use

Unknown
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG

OverviewOther

Other InhibitorOther SubstrateOther Inducer


Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
inconclusive [IC50 19.1437 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

0,9-364,5 mg administrated through intravenous infusion over 3 hours
Route of Administration: Intravenous
AZD-6482 is a potent, selective and ATP competitive PI3Kβ inhibitor (IC(50) 0.01 uM). A maximal anti-platelet effect was achieved at 1 uM in the in vitro. AZD-6482 was more potent in human blood than in dog and rat blood with IC50 values of 0.27, 1.4 and 1.8 uM in human, dog and rat blood, respectively. AZD-6482 concentration-dependently inhibited insulin-induced glucose uptake by human adipocytes in vitro with an IC50 value of 4.4 ±0.8 uM
Substance Class Chemical
Created
by admin
on Sat Dec 16 13:06:40 GMT 2023
Edited
by admin
on Sat Dec 16 13:06:40 GMT 2023
Record UNII
78G6MP5PZ5
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
AZD-6482
Common Name English
2-(((1R)-1-(7-METHYL-2-(4-MORPHOLINYL)-4-OXO-4H-PYRIDO(1,2-A)PYRIMIDIN-9-YL)ETHYL)AMINO)BENZOIC ACID
Systematic Name English
AZD6482
Code English
AZD 6482 [WHO-DD]
Common Name English
Code System Code Type Description
DRUG BANK
DB14980
Created by admin on Sat Dec 16 13:06:41 GMT 2023 , Edited by admin on Sat Dec 16 13:06:41 GMT 2023
PRIMARY
PUBCHEM
44137675
Created by admin on Sat Dec 16 13:06:41 GMT 2023 , Edited by admin on Sat Dec 16 13:06:41 GMT 2023
PRIMARY
ChEMBL
CHEMBL2165191
Created by admin on Sat Dec 16 13:06:41 GMT 2023 , Edited by admin on Sat Dec 16 13:06:41 GMT 2023
PRIMARY
CAS
1173900-33-8
Created by admin on Sat Dec 16 13:06:41 GMT 2023 , Edited by admin on Sat Dec 16 13:06:41 GMT 2023
PRIMARY
FDA UNII
78G6MP5PZ5
Created by admin on Sat Dec 16 13:06:41 GMT 2023 , Edited by admin on Sat Dec 16 13:06:41 GMT 2023
PRIMARY
EPA CompTox
DTXSID00657619
Created by admin on Sat Dec 16 13:06:41 GMT 2023 , Edited by admin on Sat Dec 16 13:06:41 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY