AZ0108
1 Cited Publications
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Based on 1 publication(s) in Google Scholar
AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models.
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- CAS No.: 1825345-52-5
- Formula: C24H20F4N6O2
- Molecular Weight:500.45
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Publications Citing Use of MedChemExpress (MCE) AZ0108
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Biological Activity
Description
AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models[1].
IC50 & Target
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PARP1 0.03 μM (IC50) |
PARP2 0.03 μM (IC50) |
PARP6 0.083 μM (IC50) |
PARP3 2.8 μM (IC50) |
TNKS1 3.2 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1806 | EC50 |
30 nM
Compound: 14f; AZ0108
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Inhibition of PARP in human HCC1806 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human HCC1806 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
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[PMID: 26546219] |
| HeLa | EC50 |
0.053 μM
Compound: 14f; AZ0108
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Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human HeLa cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
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[PMID: 26546219] |
| HeLa | EC50 |
0.053 μM
Compound: 15; AZ0108
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Inhibition of PARP in human HeLa cells assessed as induction of centrosomal clustering blockade by measuring increase in mitotic cells with multipolar spindles measured after 48 hrs by DAPI staining-based assay
Inhibition of PARP in human HeLa cells assessed as induction of centrosomal clustering blockade by measuring increase in mitotic cells with multipolar spindles measured after 48 hrs by DAPI staining-based assay
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[PMID: 27578247] |
| MCF7 | EC50 |
123 nM
Compound: 14f; AZ0108
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Inhibition of PARP in human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
Inhibition of PARP in human MCF7 cells assessed as induction of centrosome declustering after 48 hrs by DAPI-staining based image analysis
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[PMID: 26546219] |
| OCI-LY19 | GI50 |
0.017 μM
Compound: 14f; AZ0108
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Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay
Cytotoxicity against human OCI-LY19 assessed as growth inhibition after 3 days by Alamar Blue assay
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[PMID: 26546219] |
| Sf9 | IC50 |
<0.03 μM
Compound: 14f; AZ0108
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Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of full length human PARP1 expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
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[PMID: 26546219] |
| Sf9 | IC50 |
<0.03 μM
Compound: 14f; AZ0108
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Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human PARP2 (2 to 583 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
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[PMID: 26546219] |
| Sf9 | IC50 |
>3 μM
Compound: 14f; AZ0108
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Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human TNKS2 (667 to 1166 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
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[PMID: 26546219] |
| Sf9 | IC50 |
0.083 μM
Compound: 14f; AZ0108
|
Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of full length human PARP6 expressed in a Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
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[PMID: 26546219] |
| Sf9 | IC50 |
3.2 μM
Compound: 14f; AZ0108
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Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
Inhibition of human TNKS1 (1001 to 1327 residues) expressed in Baculovirus infected Sf9 insect cells using activated DNA as substrate after 1 hr by streptavidin-horseradish peroxidase-based luminescence assay
|
[PMID: 26546219] |
Chemical Information
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CAS No. 1825345-52-5
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Appearance Solid
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Molecular Weight 500.45
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Formula C24H20F4N6O2
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Color White to off-white
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SMILES
O=C(C1=CC(C(F)(C(C2=CC=CC=C23)=NNC3=O)F)=CC=C1)N4CC5=NN=C(C(F)(C)F)N5C[C@@H]4C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Pomalidomide promotes macrophage control of Mycobacterium tuberculosis via enhancing HDAC6-mediated autophagy. [Abstract]2025 Jun 17:158:114831. PMID: 40373598
Purity & Documentation
Select Batch:
Purity:
99.98%
Assay:
99.98%
ee.:
99.98%
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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