AZD 5582
AZD 5582 性质
| 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：30mg/mL； DMSO：15mg/mL；乙醇：30mg/mL |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | 12.99±0.40(Predicted) |
| 颜色 | 白色至黄色 |
AZD 5582 用途与合成方法
|
cIAP1 15 nM (IC 50 ) |
cIAP2 21 nM (IC 50 ) |
XIAP 15 nM (IC 50 ) |
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. |
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 |
AZD 5582 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-12600 | AZD 5582 | 1258392-53-8 | 2mg | 660 |
| 2024-11-08 | HY-12600 | AZD 5582 | 1258392-53-8 | 5mg | 990 |
