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AZD5582 acetate (1258392-53-8 free base) 是一种 IAP 抑制剂,与 BIR3 结构域 cIAP1、cIAP2 和 XIAP 结合,IC50 分别为 15、21 和 15 nM。 AZD5582 诱导细胞凋亡。
AZD5582 acetate (1258392-53-8 free base) 是一种 IAP 抑制剂,与 BIR3 结构域 cIAP1、cIAP2 和 XIAP 结合,IC50 分别为 15、21 和 15 nM。 AZD5582 诱导细胞凋亡。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
2 mg | ¥ 594 | 5日内发货 | |
5 mg | ¥ 891 | 5日内发货 | |
10 mg | ¥ 1,627 | 5日内发货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,870 | 5日内发货 |
产品描述 | AZD5582 acetate is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis. |
靶点活性 | CIAP1:15 nM, XIAP:15 nM, CIAP2:21 nM |
体外活性 | AZD5582 (20 nM; 48 hours) inhibited cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells[2]. AZD5582 (20 nM; 48 hours) involves in apoptosis due to induction of cell death and active caspase-3/ -8 activities by AZD5582 and IFNγ co-treatment in HCC827 NSCLC cells[2]. AZD5582 (20 nM; 17 or 25 hours) down-regulates cIAP-1, activates RIPK1( upstream regulator of caspase-8), and triggers the activation of extrinsic (caspase-8) and intrinsic (caspase-9) apoptosis pathways, causing the cleavage of caspase-3 and caspase-7[2]. |
体内活性 | AZD5582 (intravenous injection; 0.1-3.0 mg/kg; once a week; 2 weeks) causes degradation of cIAP1 and caspase 3 cleavage in tumor cells, and after a two-week treatment, the tumors largely resolved. When the mice are given a medium dose (0.5 mg/kg) of AZD5582, cIAP1 degrades after administration, but it takes a while time to reach apoptosis-inducing effect[1]. |
分子量 | 1075.36 |
分子式 | C60H82N8O10 |
Smiles | C[C@H](NC)C(N[C@H](C(N1CCC[C@H]1C(N[C@@H]2[C@H](OCC#CC#CCO[C@@H]3CC4=CC=CC=C4[C@@H]3NC([C@@H]5CCCN5C([C@@H](NC([C@@H](NC)C)=O)C6CCCCC6)=O)=O)CC7=CC=CC=C27)=O)=O)C8CCCCC8)=O.CC(O)=O |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 55 mg/ml (51.15 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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