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Chemical Structure| 1071992-99-8 Chemical Structure| 1071992-99-8

Structure of Xevinapant
CAS No.: 1071992-99-8

Chemical Structure| 1071992-99-8

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Xevinapant (AT-406) is an effective, orally bioavailable Smac mimetic, acting as an antagonist of IAPs, capable of inhibiting XIAP, cIAP1, and cIAP2 proteins with Ki values of 66.4, 1.9, and 5.1 nM, respectively.

Synonyms: AT-406; Debio 1143; ARRY-334543

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Product Details of Xevinapant

CAS No. :1071992-99-8
Formula : C32H43N5O4
M.W : 561.71
SMILES Code : O=C([C@@H]1CC[C@@](CCN(C(CC(C)C)=O)C[C@@H]2NC([C@@H](NC)C)=O)([H])N1C2=O)NC(C3=CC=CC=C3)C4=CC=CC=C4
Synonyms :
AT-406; Debio 1143; ARRY-334543
MDL No. :MFCD22124467
InChI Key :LSXUTRRVVSPWDZ-MKKUMYSQSA-N
Pubchem ID :25022340

Safety of Xevinapant

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • cIAP

    cIAP2-BIR3, Ki:5.1 nM

    cIAP1-BIR3, Ki:1.9 nM

  • XIAP

    XIAP-BIR3, Ki:66.4 nM

In Vitro:

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. PMC8419049
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. PMC8419049
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. PMC7385130
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. PMC6294826
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. PMC6294826
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. PMC6294826
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. PMC6294826
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. PMC6294826

In Vivo:

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. PMC6294826

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT06463184 Recurrent High-grade Glioma PHASE1 WITHDRAWN 2025-06-27 -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.90mL

1.78mL

0.89mL

17.80mL

3.56mL

1.78mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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