AZD5582

Catalog No.S7362

AZD5582 Chemical Structure

Molecular Weight(MW): 1015.29

AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15

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Biological Activity

Description AZD5582, a novel small-molecule IAP inhibitor, binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15
Targets
cIAP1 [1]
(Cell-free assay)
XIAP [1]
(Cell-free assay)
cIAP2 [1]
(Cell-free assay)
15 nM 15 nM 21 nM
In vitro

Human pancreatic cancer cells display different sensitivities to the synthetic IAP antagonist, AZD5582. Treating human pancreatic cancer cells with AZD5582 differentially induces apoptosis, dependent on the expression of p-Akt and p-XIAP. It targets cIAP1 to induce TNF-α-induced apoptosis. AZD5582 induces a decrease of Mcl-1 protein, a member of the Bcl-2 family, but not that of Bcl-2 and Bcl-xL[1]. HNSCC (head and neck squamous cell carcinoma) cell lines SCC25, Cal27, and FaDu show a dose-dependent cytotoxic effect after treatment with AZD5582[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 cells  NGDPc5lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFTnR241QCCq Mke0RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IHfyc5d1cCCrbnjpZol1cW:wIHHmeIVzKDR6IHjyd{BjgSCDbHHtZZIhSmy3ZTDhd5NigSxiR1m1NF03\S1yNTFOwG0> MYqyOFMzODl7OB?=
BT549 cells NV3Rc5U6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{\YSWdzd3e2aDDpcohq[mm2aX;uJI9nKGi3bXHuJGJVPTR7IHPlcIx{ MUOyOFMzODl7OB?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
XIAP; 

PubMed: 26314849     


BxPC-3, Capan-2 (upper panel), Panc-1 and AsPC-1 (lower panel) were treated with the indicated doses of AZD5582 and the cell lysates were then immunoblotted using XIAP and γ-tubulin antibodies. γ-tubulin was used as a loading control.

26314849
In vivo After AZD5582 treatment, tumor growth and weight decrease, whereas cleaved caspase 3 expression increases in Panc-1-derived xenograft model[1]. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Following a modest 0.5 mg/kg intravenous bolus dose of AZD5582 in mice, unbound plasma levels remain above the concentrations at which apoptosis induction and cell death are observed in MDA-MB-231 cells over the course of several hours. Although cIAP1 degradation happens very quickly upon exposure to AZD5582 in vivo, apoptosis induction (as measured by the amount of cleaved caspase-3) takes longer to reach a maximal effect. A single agent AZD5582 does not exhibit broad-based cytotoxicity but instead should be employed in selected tumor settings expected to be sensitive to IAP inhibitors or in rational combinations with other targeted therapies. The dihydrochloride salt of AZD5582 has sufficient aqueous solubility (>7 mg/mL at pH 4−6) to enable formulation for intravenous administration at the projected efficacious doses. With respect to chemical stability, AZD5582 is found to be photostable and hydrolytically stable between pH 4−6, although some amide hydrolysis is observed under strongly acidic (pH < 1) and basic (pH > 8) conditions. In addition, the compound is stable in the plasma of multiple species, with no compound degradation observed after several hours under physiological conditions[3].

Protocol

Cell Research:

[1]

- Collapse
  • Cell lines: The human pancreatic cancer cell lines including BxPC-3, Miapaca-2, Panc-1, Panc0813, PL45, Capan-1, Capan-2 and AsPC-1
  • Concentrations: 0, 0.01, 0.1, 0.5 μM
  • Incubation Time: 72 h
  • Method:

    DNA or siRNA-transfected or AZD5582-treated cells are collected and cell death is determined by trypan blue exclusion using at least 200∼500 cells. For the MTS assay, pancreatic cancer cells are seeded at 1∼3 × 104 cells/well in a 96-well microtiter plate. The following day, cells are treated with AZD5582, an IAP antagonist, with various doses for 72 h. The MTS assay is performed according to the MTS assay protocol 


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • Animal Models: Xenograft tumor (in Balb/c nude mice)
  • Formulation: --
  • Dosages: 3 mg/kg
  • Administration: i.v.
    (Only for Reference)

Solubility (25°C)

In vitro Water 100 mg/mL (98.49 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 1015.29
Formula

C58H78N8O8

CAS No. 1258392-53-8
Storage powder
in solvent
Synonyms N/A

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IAP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID