ASTX660

For research use only.

Catalog No.S8681

ASTX660 Chemical Structure

CAS No. 1799328-86-1

ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.

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Biological Activity

Description ASTX660 is a potent, non-peptidomimetic antagonist of cIAP1/2 and XIAP that inhibits the interactions between a SMAC-derived peptide and the BIR3 domains of XIAP (BIR3-XIAP) and cIAP1 (BIR3-cIAP1) with IC50 values less than 40 and 12 nmol/L, respectively.
Targets
cIAP2 [1]
()
cIAP1 [1]
(Cell-free assay)
XIAP [1]
(Cell-free assay)
12 nM 40 nM
In vitro

ASTX660 induces proteasomal degradation of cIAP1 and 2, resulting in downstream effects of NIK stabilization and activation of noncanonical NF-kB signaling, demonstrating cIAP1/2 antagonism. Because of their roles in the evasion of apoptosis, inhibitor of apoptosis proteins (IAP) are considered attractive targets for anticancer therapy. Treatment with ASTX660 leads to TNFa-dependent induction of apoptosis in various cancer cell lines in vitro.[1]

In vivo

ASTX660 is orally bioavailable in mice and demonstrates prolonged antagonism of XIAP and cIAP1 in vivo. ASTX660 dosing in mice bearing breast and melanoma tumor xenografts causes growth inhibition of MDA-MB-231 and A375 xenograft tumors in vivo.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: MDA-MB-231, HEK293, A375, SK-MEL-28, WSU-DLCL2
  • Concentrations: 1 nM - 10 μM
  • Incubation Time: 5 min - 4 h
  • Method:

    Live cell imaging. Cells are incubated with ASTX660 in 0.1% (v/v) DMSO, with or without neutralizing anti-TNFa antibody for 5 days, and live images are taken every 3 hours using a 10× objective.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: male BALB/c wild type mice, male SCID mice with MDA-MB-231 xenografts, male nude mice with A375 xenografts
  • Dosages: 5, 10, 20 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (185.29 mM)
Ethanol 100 mg/mL (185.29 mM)
Water Insoluble

* 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 539.68
Formula

C30H42FN5O3

CAS No. 1799328-86-1
Storage powder
in solvent
Synonyms N/A
Smiles CC1CN(C(CN1)CN2CCOCC2C)CC(=O)N3CC(C4=C3C=C(C(=N4)CO)CC5=CC=C(C=C5)F)(C)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04411030 Recruiting Drug: ASTX660|Drug: Midazolam|Drug: Itraconazole Healthy Volunteer Astex Pharmaceuticals Inc. May 20 2020 Phase 1
NCT02503423 Recruiting Drug: ASTX660 Solid Tumors|Lymphoma Astex Pharmaceuticals Inc. July 2015 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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IAP Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID