AZ-6102
货号：
IA3870
品牌：
Jinpan
暂无详情
产品简介
| 别名 | AZ6102 |
| CAS | 1645286-75-4 |
| 分子式 | C25H28N6O |
| 分子量 | 428.53 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | 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]. |
| 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 |
| 靶点 | PARP；TNKS1，TNKS2 |
| 动物实验 | 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]. |
| 数据来源文献 | [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. |
| 规格 | 5mg 10mg |
AZ6102是有效的TNKS1/2抑制剂。