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AZD5582 acetate (1258392-53-8 free base)

Catalog No. T14378L CAS T14378L

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

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AZD5582 acetate (1258392-53-8 free base), CAS T14378L

Pack Size	Availability	Price/USD
2 mg	In stock	$ 89.00
5 mg	In stock	$ 128.00
10 mg	In stock	$ 189.00

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Purity: 97.76%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	AZD5582 acetate is an inhibitor of IAPs, which binds to the BIR3 domains cIAP1, cIAP2, and XIAP with IC50s of 15, 21, and 15 nM, respectively. AZD5582 induces apoptosis.
Targets&IC50	cIAP2:21 nM, XIAP:15 nM, cIAP1:15 nM
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	1075.36
Formula	C60H82N8O10
CAS No.	T14378L

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 55 mg/ml (51.15 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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Keywords

AZD5582 acetate (1258392-53-8 free base) T14378L Apoptosis IAP AZD-5582 acetate (1258392-53-8 free base) AZD5582 acetate (1258392538 free base) AZD5582 acetate (1258392 53 8 free base) Inhibitor inhibitor inhibit

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