CAS 1645286-75-4|AZ 6102
Introduction：Basic information about CAS 1645286-75-4|AZ 6102, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | AZ 6102 | ||
|---|---|---|---|
| CAS Number | 1645286-75-4 | Molecular Weight | 428.529 |
| Density | 1.3±0.1 g/cm3 | Boiling Point | / |
| Molecular Formula | C25H28N6O | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | 2-(4-{6-[(3R,5S)-3,5-Dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl}phenyl)-7-methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one |
|---|---|
| Synonym | More Synonyms |
AZ 6102 BiologicalActivity
| Description | AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively, and alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively. |
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| Related Catalog | Research Areas >>Cancer |
| Target | TNKS2:2 nM (IC50) TNKS1:3 nM (IC50) PARP1:2 μM (IC50) PARP2:0.5 μM (IC50) |
| In Vitro | AZ6102 is a potent dual TNKS1 and TNKS2 inhibitor, with IC50s of 3 nM and 1 nM, respectively. AZ6102 alao has 100-fold selectivity against other PARP family enzymes, with IC50s of 2.0 μM, 0.5 μM, and >3 μM, for PARP1, PARP2, and PARP6, respectively. AZ6102 shows Wnt pathway inhibition in DLD-1 cells[1]. |
| Kinase Assay | 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. |
Chemical & Physical Properties
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C25H28N6O |
| Molecular Weight | 428.529 |
| Exact Mass | 428.232452 |
| LogP | 2.81 |
| Index of Refraction | 1.694 |
| Storage condition | -20℃ |
Synonyms
| 4H-Pyrrolo[2,3-d]pyrimidin-4-one, 2-[4-[6-[(3R,5S)-3,5-dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl]phenyl]-3,7-dihydro-7-methyl- |
| 2-(4-{6-[(3R,5S)-3,5-Dimethyl-1-piperazinyl]-4-methyl-3-pyridinyl}phenyl)-7-methyl-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one |
| AZ-6102 |
| AZ6102 |
