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AZ6102

Catalog No.GC16725

AZ6102 est un puissant inhibiteur double de TNKS1 et TNKS2, avec des IC50 de 3 nM et 1 nM, respectivement, et a également une sélectivité 100 fois supérieure contre d'autres enzymes de la famille PARP, avec des IC50 de 2,0 μM, 0,5 μM et> 3 μM, pour PARP1 , PARP2 et PARP6, respectivement.

Products are for research use only. Not for human use. We do not sell to patients.

AZ6102 Chemical Structure

Cas No.: 1645286-75-4

Taille Prix Stock Qté
5mg
70,00 $US
En stock
25mg
230,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment:

The assay is conducted using 0.11 μM of tankyrase-1 protein and 3 μM nicotinamide adenine dinucleotide (NAD+, 2.12 μM 3H-NAD+ with a specific radioactivity of 1690 Ci/mol, 0.88 μM biotin- NAD+), in pH 7.5 Tris buffer (60 mM Tris, 1 mM DTT, 0.01% (v/v) Tween-20®, 2.5 mM MgCl2, 0.3 mg/mL BSA). For IC50 determination, 10 mM DMSO stock solution of a compound (AZ6102) is sequentially diluted by two-fold in DMSO, and aliquots of the diluted solutions are transferred to 384-well assay plates and mixed with Tankyrase-1 solution[1].

References:

[1]. Johannes JW, et al. Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology. ACS Med Chem Lett. 2015 Jan 13;6(3):254-9.

Background

IC50: 1 and 3 nM for TNKS2 and TNKS1, respectively

AZ6102 is a TNKS1/2 inhibitor.

Inhibition of the poly(ADP-ribose) polymerase (PARP) catalytic domain of the tankyrases (TNKS1 and TNKS2) is reported to inhibit the Wnt pathway by increasing stabilization of Axin. The canonical Wnt pathway plays a critical role in adult tissue homeostasis, embryonic development, as well as cancer.

In vitro: AZ6102 was identified as a potent TNKS1/2 inhibitor with 100-fold selectivity against other PARP family enzymes including PARPs 1, 2, and 6. In addition, AZ6102 showed a 5 nM IC50 against Wnt pathway in DLD-1 cells [1].

In vivo: In animal study, AZ6102 was intravenously dosed to nude mice at 25 mg/kg, and the results showed that AZ6102 had a clearance of 24 mL/min·kg and a half-life of 4 h. The bioavailability of AZ6102 in mouse and rat was only moderate at 12% and 18%, respectively. In addition, AZ6102 was used as an intravenous probe compound to evaluate the in vivo effects of TNKS1/2 inhibition on normal tissue and tumor xenografts, however, the results of such experiments have not be released so far [1].

Clinical trial: Up to now, AZ6102 is still in the preclinical development stage.

Reference:
[1] J.  W. Johannes, L. Almeida, B. Barlaam,et al.Pyrimidinone nicotinamide mimetics as selective tankyrase and Wnt pathways inhibitors suitable for in vivopharmacology. ACS Med. Chem. Lett. 6, 254-259 (2015).

Chemical Properties

Cas No. 1645286-75-4 SDF
Chemical Name 2-(4-(6-((3S,5R)-3,5-dimethylpiperazin-1-yl)-4-methylpyridin-3-yl)phenyl)-7-methyl-3H-pyrrolo[2,3-d]pyrimidin-4(7H)-one
Canonical SMILES O=C1NC(C2=CC=C(C3=CN=C(N4C[C@H](C)N[C@H](C)C4)C=C3C)C=C2)=NC5=C1C=CN5C
Formula C25H28N6O M.Wt 428.53
Solubility DMF: 15 mg/ml,DMF:PBS(pH7.2) (1:2): 0.3 mg/ml,DMSO: 10 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.3336 mL 11.6678 mL 23.3356 mL
5 mM 0.4667 mL 2.3336 mL 4.6671 mL
10 mM 0.2334 mL 1.1668 mL 2.3336 mL
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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