AZD5582 dihydrochloride 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 dihydrochloride is an antagonist of the inhibitor ofapoptosisproteins (IAPs), which binds to the BIR3 domainscIAP1, cIAP2, andXIAPwithIC50s of 15, 21, and 15 nM, respectively. AZD5582 inducesapoptosis[1]. |
| IC50& Target[1] | cIAP1 15 nM (IC50) | cIAP2 21 nM (IC50) | XIAP 15 nM (IC50) |
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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[2].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[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].
Cell Viability Assay[2] | 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[2] | 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[2] | 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. |
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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[1].
| Animal Model: | MDA-MB-231 xenograft-bearing mice[1] | | 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 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(45.95 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 0.9189 mL | 4.5947 mL | 9.1894 mL | | 5 mM | 0.1838 mL | 0.9189 mL | 1.8379 mL | | 10 mM | 0.0919 mL | 0.4595 mL | 0.9189 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.30 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (2.30 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (2.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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