AZ0108

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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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AZ0108 Chemical Structure

CAS No. : 1825345-52-5

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

Biological Activity
Purity & Documentation
References
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Description

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)

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: 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]
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]
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]

Molecular Weight

500.45

Formula

C₂₄H₂₀F₄N₆O₂

CAS No.

1825345-52-5

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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]

AZ0108 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZ01081825345-52-5AZ 0108AZ-0108PARPpoly ADP ribose polymerasedeclusteringCentrosomeInhibitorinhibitorinhibit

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