CAS:1645286-75-4
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
AZ6102是有效的TNKS1/2抑制剂。
Array ( [133] => Array ( [id] => 133 [name] => Inhibitors & Antagonists & Agonists [num] => [children] => Array ( [352] => Array ( [id] => 352 [name] => Protein Tyrosine Kinase/PTK ) [350] => Array ( [id] => 350 [name] => PI3K/Akt/mTOR ) [351] => Array ( [id] => 351 [name] => Endocrinology & Hormones ) [357] => Array ( [id] => 357 [name] => Angiogenesis ) [358] => Array ( [id] => 358 [name] => HIF ) [363] => Array ( [id] => 363 [name] => Immunology & Inflammation ) [364] => Array ( [id] => 364 [name] => Stem Cells ) [365] => Array ( [id] => 365 [name] => Apoptosis ) [377] => Array ( [id] => 377 [name] => Metabolic Enzyme & Protease ) [379] => Array ( [id] => 379 [name] => Autophagy ) [380] => Array ( [id] => 380 [name] => ER Stress ) [384] => Array ( [id] => 384 [name] => Cell Cycle ) [385] => Array ( [id] => 385 [name] => Cytoskeleton ) [386] => Array ( [id] => 386 [name] => DNA Damage & DNA Repai ) [387] => Array ( [id] => 387 [name] => Epigenetics ) [388] => Array ( [id] => 388 [name] => Ubiquitin ) [389] => Array ( [id] => 389 [name] => JAK/STAT ) [390] => Array ( [id] => 390 [name] => GPCR & G Protein ) [391] => Array ( [id] => 391 [name] => Neuronal Signal Pathway ) [392] => Array ( [id] => 392 [name] => MAPK ) [393] => Array ( [id] => 393 [name] => NF-κB ) [394] => Array ( [id] => 394 [name] => Membrane Transporter & Ion Channel ) [395] => Array ( [id] => 395 [name] => TGF-β/Smad ) [396] => Array ( [id] => 396 [name] => Hippo ) [775] => Array ( [id] => 775 [name] => Antibody-drug Conjugate/ADC Related ) [122] => Array ( [id] => 122 [name] => Others ) ) ) )
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AZ-6102CAS:1645286-75-4
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:≥98%
Appearance:Light yellow to yellow Solid
CAS | 1645286-75-4 |
English Name | AZ-6102 |
Synonyms | Org-2969 |
Molecular Formula | C25H28N6O |
Molecular Weight | 428.53 |
Solubility | Soluble in DMSO |
Purity | ≥98% |
Appearance | Light yellow to yellow Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
MDL | MFCD28502279 |
SMILES | O=C1C2=C(N(C)C=C2)N=C(C3=CC=C(C4=C(C)C=C(N5C[C@@H](C)N[C@@H](C)C5)N=C4)C=C3)N1 |
Target Point | PARP;TNKS1,TNKS2 |
Passage | Cell Cycle;DNA Damage/DNA Repair; Epigenetics |
Background | AZ6102 is a potent TNKS1/2 inhibitor. |
Biological Activity | 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.[1] |
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]. |
Cell 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]. |
Data Literature Source | [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. |
Unit | Bottle |
Specification | 5mg 10mg |
AZ6102是有效的TNKS1/2抑制剂。