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AZD5582 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AZD5582 dihydrochloride图片
CAS NO:1883545-51-4
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

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 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)

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.
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
分子量

1088.21

性状

Solid

Formula

C58H80Cl2N8O8

CAS 号

1883545-51-4

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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM0.9189 mL4.5947 mL9.1894 mL
5 mM0.1838 mL0.9189 mL1.8379 mL
10 mM0.0919 mL0.4595 mL0.9189 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。

    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-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。

    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。

*以上所有助溶剂都可在本网站选购。