AZD 5582
| 中文名称 | AZD 5582 |
|---|---|
| 中文同义词 | 二聚化SMAC MIMETICS,IAPS抑制剂;(2S,2'S)-1,1'-((S,2S,2'S)-2,2'-(((1S,1'S,2R,2'R)-(己-2,4-二炔-1,6-二基双(氧))双(2,3-二氢-1H-茚-2,1-二基))双(环己烷-3,1-二基))双(2-((S)-2-(甲胺基)丙胺基)乙酰基)双(吡咯烷-2-甲酰胺) |
| 英文名称 | AZD-5582 |
| 英文同义词 | AZD-5582;3,3'-[2,4-Hexadiyne-1,6-diylbis[oxy[(1S,2R)-2,3-dihydro-1H-indene-2,1-diyl]]]bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-L-prolinamide];AZD5582;AZD-5582;AZD 5582;CS-2673;(S,S,2S,2'S)-N,N'-((1S,1'S,2R,2'R)-(hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(1-((S)-2-cyclohexyl-2-((S)-2-(methylamino)propanamido)acetyl)pyrrolidine-2-carboxamide);L-Prolinamide, 3,3'-[2,4-hexadiyne-1,6-diylbis[oxy[(1S,2R)-2,3-dihydro-1H-indene-2,1-diyl]]]bis[N-methyl-L-alanyl-(2S)-2-cyclohexylglycyl-;ZD5582;(2S,2'S)-1,1'-((S,2S,2'S)-2,2'-(((1S,1'S,2R,2'R)-(Hexa-2,4-diyne-1,6-diylbis(oxy))bis(2,3-dihydro-1H-indene-2,1-diyl))bis(cyclohexane-3,1-diyl))bis(2-((S)-2-(methylamino)propanamido)acetyl))bis(pyrrolidine-2-carboxamide) |
| CAS号 | 1258392-53-8 |
| 分子式 | C58H78N8O8 |
| 分子量 | 1015.29 |
| EINECS号 | |
| 相关类别 | 细胞生物学试剂;抑制剂 |
| Mol文件 | 1258392-53-8.mol |
| 结构式 |  |
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) |
|
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 |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-12600 | AZD 5582 AZD5582 | 1258392-53-8 | 2mg | 660元 |
| 2024/01/25 | HY-12600 | AZD 5582 AZD5582 | 1258392-53-8 | 5mg | 990元 |