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AZ6102 PPAR inhibitor

Name: AZ6102
Brand: Selleck Chemicals
SKU: S7767
Availability: InStock
Rating: 5 (6 reviews)

Cat.No.S7767

AZ6102 is a potent TNKS1/2 inhibitor that has 100-fold selectivity against other PARP family enzymes and shows IC50 of 5 nM for Wnt pathway inhibition in DLD-1 cells.

Chemical Structure

Molecular Weight: 428.53

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.82%

99.82

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Chemical Information, Storage & Stability

Molecular Weight	428.53	Formula	C₂₅H₂₈N₆O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1645286-75-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AZ-6102			Smiles	CC1CN(CC(N1)C)C2=NC=C(C(=C2)C)C3=CC=C(C=C3)C4=NC5=C(C=CN5C)C(=O)N4

Solubility

In vitro
Batch:

DMSO : 85 mg/mL (198.35 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (1.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.625mg/ml (1.46mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	TNKS1 ^[1] TNKS2 ^[1]
In vitro	AZ6102 inhibits TNKS1 and TNKS2 in enzymatic assays and TCF4 reporter assays (<5nM). This compound inhibits proliferation of Colo320DM (GI50 ~40nM), but has no anti-proliferative activity in the β-catenin mutant cell line HCT-116, or the BRCA mutant cell line MDA-MB-436. In Colo320DM, it stabilizes axin2 protein and modulates Wnt target genes in a dose and time dependent manner both in vitro and in vivo^[1].
In vivo	Nude mice are administered 25 mg/kg of AZ-6102. This compound has a half-life of 4 hours and a CL of 24 mL/min.kg. Further analysis in mouse and rats shows that it has a moderate bioavailability at 12% and 18%, respectively. Western blot analysis for TNKS1, TNSK2 and Axin2 of treated DLD-1 cells shows that this chemical had qualitatively stronger and longer lasting stabilization of TNSK1, TNSK2 and Axin2 than XAV-939 at lower concentrations (at 24, 48 and 72h). It has good pharmacokinetics in preclinical species with low Caco2 efflux (to avoid possible tumor resistance mechanisms). In addition, it can be formulated in a clinically relevant intravenous solution at 20 mg/mL using SBECD as an excipient at pH4. The results of this compound used as an i.v. probe compound to explore the in vivo effects of the inhibition of TNKS1 and TNSK2 on tumor xenografts and normal tissue are forthcoming^[2].
References	[1] https://pubmed.ncbi.nlm.nih.gov/25815142/ [2] https://pubmed.ncbi.nlm.nih.gov/26396691/

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