1. Apoptosis
  2. IAP
    Apoptosis
  3. AZD5582

AZD5582 

Cat. No.: HY-12600 Purity: 98.13%
Handling Instructions

AZD5582 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.

For research use only. We do not sell to patients.

AZD5582 Chemical Structure

AZD5582 Chemical Structure

CAS No. : 1258392-53-8

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10 mM * 1 mL in DMSO USD 174 In-stock
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5 mg USD 119 In-stock
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10 mg USD 180 In-stock
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50 mg USD 550 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

AZD5582 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[1].

IC50 & Target[1]

cIAP1

15 nM (IC50)

cIAP2

21 nM (IC50)

XIAP

15 nM (IC50)

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].

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

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.
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].

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

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
Molecular Weight

1015.29

Formula

C₅₈H₇₈N₈O₈

CAS No.

1258392-53-8

SMILES

CN[[email protected]@H](C)C(N[[email protected]](C(N1[[email protected]](C(N[[email protected]]2C3=CC=CC=C3C[[email protected]]2OCC#CC#CCO[[email protected]]4[[email protected]@H](NC([[email protected]@H]5CCCN5C([[email protected]@H](NC([[email protected]](C)NC)=O)C6CCCCC6)=O)=O)C(C=CC=C7)=C7C4)=O)CCC1)=O)C8CCCCC8)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 66.25 mg/mL (65.25 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9849 mL 4.9247 mL 9.8494 mL
5 mM 0.1970 mL 0.9849 mL 1.9699 mL
10 mM 0.0985 mL 0.4925 mL 0.9849 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (2.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AZD5582AZD 5582AZD-5582IAPApoptosisInhibitorinhibitorinhibit

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AZD5582
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