Art. -Nr.: HY-15454

Xevinapant

Name: Xevinapant
Brand: MedChemExpress
SKU: HY-15454
Price: 106.00 USD
Availability: InStock
Rating: 5 (12 reviews)

(Synonyms: AT-406; Debio 1143; SM-406)

12 Cited Publications

Kundenbewertung

Based on 12 publication(s) in Google Scholar

Xevinapant (AT-406) is a potent and orally bioavailable Smac mimetic and an antagonist of IAPs, and it binds to XIAP, cIAP1, and cIAP2 proteins with K_i of 66.4, 1.9, and 5.1 nM, respectively.

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Reinheit: 99.91%
CAS. Nr.: 1071992-99-8
Formel: C₃₂H₄₃N₅O₄
Molecular Weight:561.71

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Xevinapant Chemical Structure

CAS. Nr.: 1071992-99-8

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

cIAP1

1.9 nM (Ki)

cIAP2

5.1 nM (Ki)

XIAP

66.4 nM (Ki)

Alle IAP Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
EVSA-T	EC₅₀	0.0021 μM Compound: Debio-1143	Cytotoxicity against human sensitive EVSA-T cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay Cytotoxicity against human sensitive EVSA-T cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay	[PMID: 26218264]
HCT-116	EC₅₀	>10 μM Compound: Debio-1143	Cytotoxicity against human insensitive HCT116 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay Cytotoxicity against human insensitive HCT116 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay	[PMID: 26218264]
HEK293	EC₅₀	0.034 μM Compound: Debio-1143	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 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	[PMID: 26218264]
MDA-MB-231	EC₅₀	0.019 μM Compound: Debio-1143	Cytotoxicity against human sensitive MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay Cytotoxicity against human sensitive MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay	[PMID: 26218264]
MDA-MB-231	IC₅₀	144 nM Compound: 2, SM-406	Growth inhibition of human MDA-MB-231 cells after 4 days by WST8 assay Growth inhibition of human MDA-MB-231 cells after 4 days by WST8 assay	[PMID: 21443232]
SK-OV-3	IC₅₀	142 nM Compound: 2, SM-406	Growth inhibition of human SKOV3 cells after 4 days by WST8 assay Growth inhibition of human SKOV3 cells after 4 days by WST8 assay	[PMID: 21443232]

In Vitro

Xevinapant mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. Xevinapant is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. Xevinapant (1 μM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system. In MDA-MB-231 cell, Xevinapant induces rapid cellular cIAP1 degradation and also pulls down the cellular XIAP protein. Xevinapant effectively inhibits lots of human cancer cell lines and shows IC₅₀ of 144 and 142 nM in MDA-MB-231 cell and SK-OV-3 ovarian cell, with low toxicity against normal-like human breast epithelial MCF-12F cells and primary human normal prostate epithelial cells. Xevinapant induces apoptosis in MDA-MB-231 cell by inducing activation of caspase-3 and cleavage of PARP^[1]. Xevinapant displays single agent activity in ovarian cancer cell lines. The IC₅₀ values of AT-406 in these ovarian cancer cells range from 0.05-0.5 μg/mL. Xevinapant exhibits anti-ovarian cancer efficacy both as a single agent and in combination with carboplatin. Xevinapant (30 μg/mL) induced degradation of XIAP in the drug sensitive ovarian cancer cell lines^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Xevinapant (AT-406) is very effective in inhibition of tumor growth in the MDA-MB-231 xenograft model, and has minimal toxicity to animals^[1]. Xevinapant is evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

SCID mice bearing MDA-MB-231 xenograft tumors^[1]
Dosage:

30 and 100 mg/kg
Administration:

p.o.; 5 days a week for 2 weeks
Result:

Strongly inhibits tumor growth at 30 and 100 mg/kg and completely inhibits tumor growth during the treatment with 100 mg/kg.

Chemical Information

CAS. Nr. 1071992-99-8
Appearance Solid
Molecular Weight 561.71
Formel C₃₂H₄₃N₅O₄
Color White to off-white
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
Synonyms

AT-406; Debio 1143; SM-406
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All Cell Proliferation/Viability AssayBio/Physico-chemical AssayIn Vivo Efficacy Study

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Journal Impact Factor

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 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 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 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 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 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.
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 Oct 1;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

Birc3 and Tip1 are upregulated in renal ischemia reperfusion injury. [Abstract]

2023 Aug 5:876:147492. PMID: 37209886
bioRxiv

2026 Mar 6.
bioRxiv

SMAC mimetics induce human macrophages to phagocytose live cancer cells. [Abstract]

2024 Nov 28:2024.11.25.625306. PMID: 39651304
Research Square Preprint

2024 Apr 15.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (178.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7803 mL

8.9014 mL

17.8028 mL

5 mM

0.3561 mL

1.7803 mL

3.5606 mL

10 mM

0.1780 mL

0.8901 mL

1.7803 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7803 mL	8.9014 mL	17.8028 mL	44.5070 mL
	5 mM	0.3561 mL	1.7803 mL	3.5606 mL	8.9014 mL
	10 mM	0.1780 mL	0.8901 mL	1.7803 mL	4.4507 mL
	15 mM	0.1187 mL	0.5934 mL	1.1869 mL	2.9671 mL
	20 mM	0.0890 mL	0.4451 mL	0.8901 mL	2.2253 mL
	25 mM	0.0712 mL	0.3561 mL	0.7121 mL	1.7803 mL
	30 mM	0.0593 mL	0.2967 mL	0.5934 mL	1.4836 mL
	40 mM	0.0445 mL	0.2225 mL	0.4451 mL	1.1127 mL
	50 mM	0.0356 mL	0.1780 mL	0.3561 mL	0.8901 mL
	60 mM	0.0297 mL	0.1484 mL	0.2967 mL	0.7418 mL
	80 mM	0.0223 mL	0.1113 mL	0.2225 mL	0.5563 mL
	100 mM	0.0178 mL	0.0890 mL	0.1780 mL	0.4451 mL

Bioz

Xevinapant

12 Cited Publications

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Xevinapant

Birinapant

LCL161

SM-164

Tolinapant

AZD5582

GDC-0152

BV6

CUDC-427

Navitoclax

Venetoclax

Embelin

Z-VAD-FMK

Publications Citing Use of MedChemExpress (MCE) Xevinapant

Alle IAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

Xevinapant

Birinapant

LCL161

SM-164

Tolinapant

AZD5582

GDC-0152

BV6

CUDC-427

Navitoclax

Venetoclax

Embelin

Z-VAD-FMK

Publications Citing Use of MedChemExpress (MCE) Xevinapant

Alle IAP Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Xevinapant Related Classifications

HY-15454 Related Classifications

Bioz