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Referencia número: HY-100847

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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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No. CAS: 1825345-52-5
Fòrmula: C₂₄H₂₀F₄N₆O₂
Peso molecular:500.45

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

AZ0108 Chemical Structure

No. CAS: 1825345-52-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Publications (1)
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Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

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)

Ver todos los productos específicos de isoformas PARP :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1806	EC₅₀	30 nM Compound: 14f; AZ0108	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	[PMID: 26546219]
HeLa	EC₅₀	0.053 μM Compound: 14f; AZ0108	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	[PMID: 26546219]
HeLa	EC₅₀	0.053 μM Compound: 15; AZ0108	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	[PMID: 27578247]
MCF7	EC₅₀	123 nM Compound: 14f; AZ0108	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	[PMID: 26546219]
OCI-LY19	GI₅₀	0.017 μM Compound: 14f; AZ0108	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	[PMID: 26546219]
Sf9	IC₅₀	<0.03 μM Compound: 14f; AZ0108	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	[PMID: 26546219]
Sf9	IC₅₀	<0.03 μM Compound: 14f; AZ0108	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	[PMID: 26546219]
Sf9	IC₅₀	>3 μM Compound: 14f; AZ0108	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	[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	[PMID: 26546219]
Sf9	IC₅₀	3.2 μM Compound: 14f; AZ0108	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

No. CAS 1825345-52-5
Peso molecular 500.45
Fòrmula C₂₄H₂₀F₄N₆O₂
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
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Journal Impact Factor

Int Immunopharmacol

Pomalidomide promotes macrophage control of Mycobacterium tuberculosis via enhancing HDAC6-mediated autophagy. [Abstract]

2025 Jun 17:158:114831. PMID: 40373598

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Johannes JW, et al., Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5743-7. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

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AZ0108

1 Cited Publications

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Actividad biológica
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Publications (1)
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AZ0108

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AZ0108

Ver todos los productos específicos de isoformas PARP

Actividad biológica

Chemical Information

Publications (1)

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Referencias

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Help & FAQs

AZ0108

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AZ0108

Ver todos los productos específicos de isoformas PARP

Actividad biológica

Chemical Information

Publications (1)

Pureza y Documentación

Referencias

Calculators

Help & FAQs

AZ0108 Related Classifications

HY-100847 Related Classifications