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AZD5582

Catalog No. T14378 CAS 1258392-53-8

AZD5582 is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. It induces <a href="/pathway/Apoptosis" style="display: inline; color: #c13a36">Apoptosis</a>.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

AZD5582, CAS 1258392-53-8

Pack Size	Availability	Price/USD
5 mg	In Stock (ship within 1 week)	$ 100.00
10 mg	In Stock (ship within 1 week)	$ 150.00
50 mg	In Stock (ship within 1 week)	$ 448.00
1 mL * 10 mM (in DMSO)	In Stock (ship within 1 week)	$ 227.00

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZD5582 is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. It induces apoptosis.
Targets&IC50	cIAP2:21 nM (IC50), XIAP:15 nM (IC50), cIAP1:15 nM (IC50)
In vitro	AZD5582 (20 nM; 48 hours) inhibited cell viability by cooperation with IFNγ or viral double-stranded RNA (dsRNA) in H1975 NSCLC cells[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]. AZD5582 (20 nM; 17 or 25 hours) down-regulates 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].
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].

Molecular Weight	1015.29
Formula	C58H78N8O8
CAS No.	1258392-53-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 66.25 mg/mL (65.25 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AZD5582 1258392-53-8 Apoptosis IAP AZD 5582 inhibit AZD-5582 Inhibitor inhibitor

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