AT406 is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs), AT-406 binds to XIAP, cIAP1, and cIAP2 proteins with K (i) of 66.4, 1.9, and 5.1 nM, respectively.
Xevinapant 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HIV-1-infected macrophages
1 µM
4 hours
To evaluate the toxicity of DIABLO/SMAC mimetic-loaded TNP on HIV-1-infected cells, results showed that TNP-LCL-161 and TNP-AT-406 induced dose-dependent cytotoxicity in HIV-1-infected macrophages.
Theranostics. 2021 Aug 25;11(18):9009-9021.
HIV-1-infected resting memory CD4+ T cells
100 nM
4 hours
To evaluate the toxicity of DIABLO/SMAC mimetic-loaded TNP on HIV-1-infected cells, results showed that TNP-LCL-161 and TNP-AT-406 induced dose-dependent cytotoxicity in HIV-1-infected resting memory CD4+ T cells.
Theranostics. 2021 Aug 25;11(18):9009-9021.
IGROV-1 cells
10 µM
48 and 72 hours
DEBIO 1143 was able to reverse carboplatin resistance by inducing cell death either by apoptosis or necroptosis depending on the cell lines.
Sci Rep. 2018 Dec 14;8(1):17862.
A2780S cells
10 µM
48 and 72 hours
DEBIO 1143 was able to reverse carboplatin resistance by inducing cell death either by apoptosis or necroptosis depending on the cell lines.
Sci Rep. 2018 Dec 14;8(1):17862.
A2780R cells
10 µM
48 and 72 hours
DEBIO 1143 was able to reverse carboplatin resistance by inducing cell death either by apoptosis or necroptosis depending on the cell lines.
Sci Rep. 2018 Dec 14;8(1):17862.
SKOV-3 cells
10 µM
48 and 72 hours
DEBIO 1143 was able to reverse carboplatin resistance by inducing cell death either by apoptosis or necroptosis depending on the cell lines.
Sci Rep. 2018 Dec 14;8(1):17862.
EFO-21 cells
10 µM
48 and 72 hours
DEBIO 1143 was able to reverse carboplatin resistance by inducing cell death either by apoptosis or necroptosis depending on the cell lines.
Sci Rep. 2018 Dec 14;8(1):17862.
HIV-infected macrophages
2 µM
48 hours
To evaluate the toxicity of SMAC mimetics on HIV-infected macrophages, it was found that LCL-161, AT-406, and birinapant significantly increased the cytotoxicity of HIV-Mφ, and this cell death was dependent on the TNF signaling pathway.
Cell Death Dis. 2020 Jul 27;11(7):590.
Xevinapant 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Nude mice
SKOV-3 subcutaneous and intraperitoneal tumor models
Intraperitoneal injection and Oral gavage
40 mg/kg carboplatin and 100 mg/kg DEBIO 1143
Carboplatin once a week for three weeks; DEBIO 1143 five days per week for three weeks
DEBIO 1143 alone was able to inhibit tumor growth, and in combination with carboplatin, it significantly enhanced the efficacy of carboplatin, leading to tumor growth inhibition and complete regression.
Cytotoxicity against human sensitive EVSA-T cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay, EC50=0.0021 μM
26218264
HEK293 cells
Function assay
2 h
Antagonist activity at full-length FLAG-tagged XIAP (unknown origin) transfected in HEK293 cells assessed as inhibition of interaction with caspase 9 after 2 hrs by immunoprecipitation assay, EC50=0.034 μM
26218264
human SKOV3 cells
Growth inhibition assay
4 days
Growth inhibition of human SKOV3 cells after 4 days by WST8 assay, IC50=0.142 μM
21443232
MDA-MB-231 cells
Cytotoxicity assay
72 h
Cytotoxicity against human sensitive MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay, EC50=0.019 μM
26218264
MDA-MB-231 cells
Growth inhibition assay
4 days
Growth inhibition of human MDA-MB-231 cells after 4 days by WST8 assay, IC50=0.144 μM
21443232
MDA-MB-231 cells
1.5 μM
Function assay
12 h
Induction of apoptosis in human MDA-MB-231 cells assessed as activation of PARP cleavage at 1.5 uM after 12 hrs by Western blot analysis
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