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  3. Xevinapant

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

Cat. No.: HY-15454 Purity: 99.75%
Handling Instructions

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 Ki of 66.4, 1.9, and 5.1 nM, respectively.

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

Xevinapant Chemical Structure

Xevinapant Chemical Structure

CAS No. : 1071992-99-8

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 165 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 650 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Based on 3 publication(s) in Google Scholar

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Description

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 Ki of 66.4, 1.9, and 5.1 nM, respectively.

IC50 & Target[1]

cIAP1

1.9 nM (Ki)

cIAP2

5.1 nM (Ki)

XIAP

66.4 nM (Ki)

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].

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].

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.
Clinical Trial
Molecular Weight

561.71

Formula

C₃₂H₄₃N₅O₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Methanol : 250 mg/mL (445.07 mM; Need ultrasonic)

DMSO : 100 mg/mL (178.03 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.75%

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Xevinapant
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