AZ 6102

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Cat.No. 5775 - AZ 6102 | C25H28N6O | CAS No. 1645286-75-4
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

Chemicalprobes.org 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

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Technical Data

M. Wt 428.53
Formula C25H28N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1645286-75-4
PubChem ID 91663328
InChI Key WCPTUQOMNJBIET-CALCHBBNSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

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

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

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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Cancer

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