AZ 6102

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Description: Potent TNKS1/2 inhibitor
Chemical Name: rel-2-[4-[6-[(3R,5S)-3,5-Dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl]phenyl]-3,7-dihydro-7-methyl-4H-pyrrolo[2,3-d]pyrimidin-4-one
Purity: ≥98% (HPLC)
Literature (1)

Biological Activity for AZ 6102

AZ 6102 is a potent TNKS2 and TNKS1 inhibitor (IC50 values are 1 and 3 nM, respectively). Exhibits >100-fold selectivity for TNKS1/2 over PARP-1, PARP-2 and PARP-6. Inhibits Wnt signaling in DLD-1 cells (IC50 = 5 nM). Exhibits moderate oral bioavailability.

External Portal Information for AZ 6102 is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of AZ6102 is reviewed on the chemical probes website.

Compound Libraries for AZ 6102

AZ 6102 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for AZ 6102

M. Wt 428.53
Formula C25H28N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1645286-75-4
PubChem ID 91663328
Smiles CC1=CC(N2C[C@H](C)N[C@H](C)C2)=NC=C1C3=CC=C(C(N4)=NC5=C(C=CN5C)C4=O)C=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for AZ 6102

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 21.43 50

Preparing Stock Solutions for AZ 6102

The following data is based on the product molecular weight 428.53. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.67 mL 23.34 mL 46.67 mL
2.5 mM 0.93 mL 4.67 mL 9.33 mL
5 mM 0.47 mL 2.33 mL 4.67 mL
25 mM 0.09 mL 0.47 mL 0.93 mL

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References for AZ 6102

References are publications that support the biological activity of the product.

Johannes et al (2015) Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology. ACS Med.Chem.Lett. 13 254 PMID: 25815142

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Citations for AZ 6102

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Literature in this Area

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Stem Cell Research Product Guide

Stem Cell Research Product Guide

This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:

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  • GMP and Ancillary Material Grade Products