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AZD5582 TFA

Catalog No. T36201L

Synonyms: AZD5582 TFA（1258392-53-8 free base）

AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA induces apoptosis.

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

AZD5582 TFA, CAS N/A

Pack Size	Availability	Price/USD
1 mg	In stock	$ 50.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 152.00
25 mg	In stock	$ 273.00
50 mg	In stock	$ 465.00
100 mg	In stock	$ 682.00
1 mL * 10 mM (in DMSO)	In stock	$ 147.00

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Purity: 98.83%

Biological Description

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Description	AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA induces apoptosis.
Targets&IC50	CIAP1:15 nM, CIAP2:21 nM, XIAP:15 nM
In vitro	AZD5582 TFA (20 nM; 48 h; H1975 NSCLC cell line) in collaboration with IFNγ or viral double-stranded RNA (dsRNA), suppresses cell viability and even induces cell death in H1975 NSCLC cells.[2] AZD5582 TFA (20 nM; 17 or 25 h) induces cIAP-1 downregulation, promotes RIPK1 activation (an upstream regulator of caspase-8), and initiates the activation of both extrinsic (caspase-8) and intrinsic (caspase-9) apoptotic pathways, resulting in the cleavage of caspase-3 and caspase-7.[2] AZD5582 TFA (20 nM; 48 h; H1975 NSCLC cell line) is involved in apoptosis due to induction of cell death and active caspase-3/8 activities by AZD5582 TFA and IFNγ co-treatment in HCC827 NSCLC cells.[2]
In vivo	AZD5582 TFA (0.1-3.0 mg/kg; i.v.; once a week; 2 weeks; MDA-MB-231 xenograft-bearing mice) triggers cIAP1 degradation and caspase 3 cleavage within tumor cells. Following a two-week treatment, significant tumor resolution is observed. Upon administering a medium dose of 0.5 mg/kg AZD5582 TFA to mice, cIAP1 degradation occurs upon administration, although it takes some time for the apoptosis-inducing effects to manifest.[1]

Synonyms	AZD5582 TFA（1258392-53-8 free base）
Molecular Weight	1129.31
Formula	C60H79F3N8O10

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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;56(24):9897-9919. 2. Hao Q, et al. Interferon-γ and Smac mimetics synergize to induce apoptosis of lung cancer cells in a TNFα-independent manner. Cancer Cell Int. 2018;18:84. 3. Su K, et al. EV-T synergizes with AZD5582 to overcome TRAIL resistance through concomitant suppression of cFLIP, MCL-1, and IAPs in hepatocarcinoma. J Mol Med (Berl). 2022;100(4):629-643.

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Keywords

AZD5582 TFA Apoptosis IAP 1258392-53-8 free base AZD5582 TFA（1258392-53-8 free base） 1258392-53-8 AZD5582 TFA inhibitor inhibit

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