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

Name: Xevinapant
Brand: MedChemExpress
SKU: HY-15454
Rating: 5.0 (11 reviews)

Cat. No.: HY-15454 Purity: 99.91%: Data Sheet
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Handling Instructions
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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.

For research use only. We do not sell to patients.

CAS No. : 1071992-99-8

Size	Stock	Quantity

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Xevinapant:

Xevinapant hydrochloride In-stock

11 Publications Citing Use of MCE Xevinapant

Cell Proliferation/Viability Assay

Bio/Physico-chemical Assay

In Vivo Efficacy Study

: 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.

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cIAP cIAP-1 cIAP-2 XIAP

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

cIAP1

1.9 nM (Ki)

cIAP2

5.1 nM (Ki)

XIAP

66.4 nM (Ki)

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.

Molecular Weight

561.71

Formula

C₃₂H₄₃N₅O₄

CAS No.

1071992-99-8

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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, 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

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

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.91%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (257 KB) HNMR (304 KB) LCMS (89 KB)

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]

Complete Stock Solution Preparation Table

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

Xevinapant Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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

Customer Review

Other Forms of Xevinapant:

Xevinapant Related Antibodies

11 Publications Citing Use of MCE Xevinapant

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All IAP Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Xevinapant Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Xevinapant Related Classifications

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