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
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
| 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 |
DescriptionCurator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/25042253
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.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: O00459 Gene ID: 5296.0 Gene Symbol: PIK3R2 Target Organism: Homo sapiens (Human) |
|||
| 10.0 nM [IC50] | |||
Target ID: GO:0070527 |
0.27 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Preventing | Unknown Approved UseUnknown |
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
Edited
Sat Dec 16 13:06:40 UTC 2023
by
admin
on
Sat Dec 16 13:06:40 UTC 2023
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| Record UNII |
78G6MP5PZ5
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| Record Status |
Validated (UNII)
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| Record Version |
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CHEMBL2165191
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DTXSID00657619
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TARGET -> INHIBITOR |
IC50
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |
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