AZD 5582
- CAS号:1258392-53-8
- 英文名:AZD-5582
- 中文名:AZD 5582
- CBNumber:CB52731019
- 分子式:C58H78N8O8
- 分子量:1015.29
- MOL File:1258392-53-8.mol
- 沸点 :1207.3±65.0 °C(Predicted)
- 密度 :1.26±0.1 g/cm3(Predicted)
- 储存条件 :4°C, protect from light, stored under nitrogen
- 溶解度 :DMF: 30 mg/ml; DMSO: 15 mg/ml; Ethanol: 30 mg/ml
- 形态 :A crystalline solid
- 酸度系数(pKa) :12.99±0.40(Predicted)
- 颜色 :White to yellow
AZD 5582性质、用途与生产工艺
- 生物活性 AZD5582 是 IAP 拮抗剂，可以有效与 cIAP1，cIAP2 和 XIAP 的 BIR3 结构域结合, IC50 值分别为 15，21，15 nM。AZD5582 诱导凋亡 (apoptosis)。
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靶点
cIAP1
15 nM (IC 50 )
cIAP2
21 nM (IC 50 )
XIAP
15 nM (IC 50 )
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体外研究
AZD5582 (20 nM; 48 hours) inhibits cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells. AZD5582 (20 nM; 17 or 25 hours) downregulates 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. 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.
Cell Viability Assay
Cell Line: H1975 NSCLC cell line Concentration: 20 nM Incubation Time: 48 hours Result: Cooperated with IFNγ or viral double-stranded RNA (dsRNA) to inhibit cell viability even cell death. Apoptosis Analysis
Cell Line: HCC827 NSCLC cell line Concentration: 20 nM Incubation Time: 48 hours Result: Had an inhibitory effect on cell viability by cooperating with IFNγ. Western Blot Analysis
Cell Line: H1975 NSCLC cell line Concentration: 20 nM Incubation Time: 17 or 25 hours Result: Down-regulated cIAP-1, activated RIPK1 (upstream regulator of caspase-8), triggered the cleavage (activation) of caspase-3,7,8 and 9. -
体内研究
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.
Animal Model: MDA-MB-231 xenograft-bearing mice Dosage: 0.1 mg/kg, 0.5 mg/kg, 3.0 mg/kg Administration: Intravenous injection; once a week; 2 weeks Result: Resulted in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg
- 更新日期：2024/11/08
- 产品编号：HY-12600
- 产品名称：AZD 5582 AZD5582
- CAS编号：1258392-53-8
- 包装：2mg
- 价格：660元
- 更新日期：2024/11/08
- 产品编号：HY-12600
- 产品名称：AZD 5582 AZD5582
- CAS编号：1258392-53-8
- 包装：5mg
- 价格：990元
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
