AZD5582 dihydrochloride|cas:1883545-51-4|西域试剂

AZD5582 dihydrochloride,98.67%

产品编号：Bellancom-110346| CAS NO：1883545-51-4| 分子式：C₅₈H₈₀Cl₂N₈O₈| 分子量：1088.21

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货号	价格	库存与货期
Bellancom-110346	￥1900.00	杭州北京（现货）
Bellancom-110346	￥3100.00	杭州北京（现货）
Bellancom-110346	￥6500.00	杭州北京（现货）
Bellancom-110346	￥10500.00	杭州北京（现货）

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AZD5582 dihydrochloride

产品介绍

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 of apoptosis proteins (IAPs), which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC₅₀s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 50 mg/mL (45.95 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (protect from light)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。