Xevinapant hydrochloride
Based on 12 publication(s) in Google Scholar
Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors.
For research use only. We do not sell to patients.
- Purity: 98.11%
- CAS No.: 1071992-57-8
- Formula: C32H44ClN5O4
- Molecular Weight:598.18
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Storage:
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Xevinapant hydrochloride
More- Nat Chem Biol. 2025 Aug;21(8):1238-1249. [Abstract]
- Biomark Res. 2025 Jan 9;13(1):8. [Abstract]
- J Exp Clin Cancer Res. 2025 Jul 4;44(1):191. [Abstract]
- J Med Chem. 2019 Oct 24;62(20):9188-9200. [Abstract]
- Cancer Gene Ther. 2026 May 2. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2019 Jun 26;1865(10):2618-2632. [Abstract]
- Sci Rep. 2026 Feb 11;16(1):5882. [Abstract]
- Viruses. 2021 Dec 13;13(12):2490. [Abstract]
- Gene. 2023 Aug 5:876:147492. [Abstract]
- bioRxiv. 2026 Mar 6.
- bioRxiv. 2024 Nov 28:2024.11.25.625306. [Abstract]
- Research Square Preprint. 2024 Apr 15.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
Biological Activity
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cIAP1 1.9 nM (Ki) |
cIAP2 5.1 nM (Ki) |
XIAP 66.4 nM (Ki) |
Xevinapant (AT-406) hydrochloride potently inhibits cell growth in the MDA-MB-231 breast and SK-OV-3 ovarian cancer cell lines with IC50=144 nM and 142 nM, respectively. Xevinapant (0-3 μM; 0-48 horus) hydrochloride effectively induces cell death in a time- and dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice bearing MDA-MB-231 xenograft tumors[1]
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Dosage:30 and 100 mg/kg
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Administration:p.o.; 5 days a week for 2 weeks
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Result:Strongly inhibits tumor growth at 30 and 100 mg/kg and completely inhibits tumor growth during the treatment with 100 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1071992-57-8
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Appearance Solid
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Molecular Weight 598.18
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Formula C32H44ClN5O4
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Color White to off-white
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SMILES
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.[H]Cl
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Synonyms
AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (12)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
Persistent activation of TRPM4 triggers necrotic cell death characterized by sodium overload. [Abstract]2025 Aug;21(8):1238-1249. PMID: 39915626 -
Biomark Res
SMAC-armed oncolytic virotherapy enhances the anticancer activity of PD1 blockade by modulating PANoptosis. [Abstract]2025 Jan 9;13(1):8. PMID: 39789615 -
J Exp Clin Cancer Res
The reprogramming impact of SMAC-mimetic on glioblastoma stem cells and the immune tumor microenvironment evolution. [Abstract]2025 Jul 4;44(1):191. PMID: 40616096
Xevinapant hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 4;44(1):191. [Abstract]
Cell viabilities were measured following different doses of Xevinapant (0-400 μM) in human GSC2 and GSC4.
Xevinapant hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 4;44(1):191. [Abstract]
Cell viabilities were measured following different doses of Xevinapant in mGSC.
Xevinapant hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 4;44(1):191. [Abstract]
Caspase 3/7 activity measurement following different dosing of Xevinapant (100-400 μM) in human GSCs.
Xevinapant hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 4;44(1):191. [Abstract]
Kaplan-Meier survival curves of immunocompromised mice bearing GSC2 and GSC4 treated with Vehicle or Xevinapant (50 mg/kg/day, oral, 2 weeks).
Xevinapant hydrochloride purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Jul 4;44(1):191. [Abstract]
Tumor cell and immune cell ratio in vehicle and Xevinapant tumors respectively.
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J Med Chem
Aryl-fluorosulfate-based Lysine Covalent Pan-Inhibitors of Apoptosis Protein (IAP) Antagonists with Cellular Efficacy. [Abstract]2019 Oct 24;62(20):9188-9200. PMID: 31550155 -
Cancer Gene Ther
b-AP15 enhances TRAIL-induced cell death in HNSCC via the induction of ROS/JNK/DR5 signalling. [Abstract]2026 May 2. PMID: 42069980 -
Biochim Biophys Acta Mol Basis Dis
Directed elimination of senescent cells attenuates development of osteoarthritis by inhibition of c-IAP and XIAP. [Abstract]2019 Jun 26;1865(10):2618-2632. PMID: 31251987 -
Sci Rep
Comparing and combining xevinapant with ATR and PARP inhibition for the radiosensitization of HPV-negative HNSCC cells. [Abstract]2026 Feb 11;16(1):5882. PMID: 41673235 -
Viruses
The A179L Gene of African Swine Fever Virus Suppresses Virus-Induced Apoptosis but Enhances Necroptosis. [Abstract]2021 Dec 13;13(12):2490. PMID: 34960759 -
Gene
2023 Aug 5:876:147492. PMID: 37209886 -
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bioRxiv
2024 Nov 28:2024.11.25.625306. PMID: 39651304 -
Solvent & Solubility
DMSO : 175 mg/mL (292.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 8.75 mg/mL (14.63 mM); Clear solution
This protocol yields a clear solution of ≥ 8.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (87.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 8.75 mg/mL (14.63 mM); Clear solution
This protocol yields a clear solution of ≥ 8.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (87.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Cai Q, Sun H, Peng Y, et al. A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment. J Med Chem. 2011;54(8):2714-2726. [Content Brief]
[2]. Brunckhorst MK, et al. AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer. Cancer Biol Ther. 2012;13(9):804-811. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6717 mL | 8.3587 mL | 16.7174 mL | 41.7934 mL |
| 5 mM | 0.3343 mL | 1.6717 mL | 3.3435 mL | 8.3587 mL | |
| 10 mM | 0.1672 mL | 0.8359 mL | 1.6717 mL | 4.1793 mL | |
| 15 mM | 0.1114 mL | 0.5572 mL | 1.1145 mL | 2.7862 mL | |
| 20 mM | 0.0836 mL | 0.4179 mL | 0.8359 mL | 2.0897 mL | |
| 25 mM | 0.0669 mL | 0.3343 mL | 0.6687 mL | 1.6717 mL | |
| 30 mM | 0.0557 mL | 0.2786 mL | 0.5572 mL | 1.3931 mL | |
| 40 mM | 0.0418 mL | 0.2090 mL | 0.4179 mL | 1.0448 mL | |
| 50 mM | 0.0334 mL | 0.1672 mL | 0.3343 mL | 0.8359 mL | |
| 60 mM | 0.0279 mL | 0.1393 mL | 0.2786 mL | 0.6966 mL | |
| 80 mM | 0.0209 mL | 0.1045 mL | 0.2090 mL | 0.5224 mL | |
| 100 mM | 0.0167 mL | 0.0836 mL | 0.1672 mL | 0.4179 mL |
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