AZD5582|1258392-53-8|-陌孚医药/Medlife

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AZD5582

目录号: PL02782 纯度: ≥98%

CAS No. :1258392-53-8

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中文名称	AZD5582
中文别名	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	AZD5582
英文别名	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;GTPL7710;AOB5560;(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]-N-[(1S,2R)-2-[6-[[(1S,2R)-1-[[(2S)-1-[(2S)-2-cyclohexyl-2-[[(2S)-2-(methylamino)propanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-2,3-dihydro-1H-inden-2-yl]oxy]hexa-2,4-diynoxy]-2,3-dihydro-1H-inden-1-yl]pyrrolidine-2-carboxamide;BDBM50495451;NSC787048;s7362;Q27074760;(2S)-1-[(2S)-2-cyclo;CID 49847690
Cas No.	1258392-53-8
分子式	C₅₈H₇₈N₈O₈
分子量	1015.29
包装储存	4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

产品详情	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)。
生物活性	AZD5582 is an antagonist of the inhibitor of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC 50 s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
性状	Solid
IC50 & Target[1][2]	cIAP1 15 nM (IC50) cIAP2 21 nM (IC50
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
参考文献	[1]. Hennessy EJ, et al. Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582). J Med Chem. 2013 Dec 27;56(24):9897-919. [2]. Qin Hao, et al. IF-γ and Smac mimetics synergize to induce apoptosis of lung cancer cells in a TNFα-independent manner,Cancer Cell Int. 2018; 18: 84.

溶解度数据	In Vitro: DMSO : ≥ 66.25 mg/mL (65.25 mM)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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