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Cat. No. M2026
AT-406 Structure

SM-406; Xevinapant; Debio 1143

Size Price Availability Quantity
2mg USD 60  USD60 In stock
5mg USD 105  USD105 In stock
10mg USD 155  USD155 In stock
25mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

AT-406 (formerly known as SM-406) is a novel and orally active antagonist of multiple IAP proteins. AT-406 selectively inhibits the biological activity of IAP proteins, including X chromosome-linked IAP (XIAP), the cellular IAPs 1 (c-IAP1) and 2 (c-IAP2) and melanoma inhibitor of apoptosis protein (ML-IAP). AT-406 effectively antagonizes XIAP BIR3 protein in a cell-free functional assay. AT-406 induced apoptosis is correlated with its ability to down-regulate XIAP whereas AT-406 induces cIAP1 degradation in both AT-406 sensitive and resistance cell lines. AT-406 is highly effective in induction of apoptosis in xenograft tumors, and is capable of complete inhibition of tumor growth. Additionally, AT-406 enhances the carboplatin-induced ovarian cancer cell death and increases survival of the experimental mice in vivo. AT-406 is currently in phase I clinical trials for the treatment of human cancer.

Customer Product Validations & Biological Datas
Source J Pharmacol Sci (2014). Figure 1. AT-406
Method CCK-8 analysis
Cell Lines Hela cells and Siha cells
Concentrations 24 h
Incubation Time 5 or 10 μM
Results The results of CCK-8 analysis showed that AT-406 cell inhibition was less than 20% at these concentrations. Under normoxic and hypoxic conditions, Hela cells treated with AT-406 at 10 μM prior to irradiation showed a significant survival curve shift with SERs of 1.81 and 2.07, respectively, compared with untreated Hela cells
Protocol (for reference only)
Cell Experiment
Cell lines MDA-MB-231 breast cancer and SK-OV-3 ovarian cancer cell lines
Preparation method The MDA-MB-231 breast cancer and SK-OV-3 ovarian cancer cell lines were purchased from the American Type Culture Collection (ATCC). Cells were seeded in 96-well flat bottom cell culture plates at a density of 3–4×103 cells/well with compounds and incubated for 4 days. The rate of cell growth inhibition after treatment with different concentrations of the inhibitors was determined by assaying with (2-(2-methoxy-4-nitrophenyl)-3-(4-nitrophenyl)-5-(2,4-disulfophenyl)-2H-tetrazolium mono-sodium salt. WST-8 was added to each well to a final concentration of 10%, and then the plates were incubated at 37°C for 2–3 h. The absorbance of the samples was measured at 450 nm using a TECAN ULTRA Reader. Concentration of the compounds that inhibited cell growth by 50% (IC50) was calculated by comparing absorbance in the untreated cells and the cells treated with the compounds.
Concentrations 0~3000 nM
Incubation time 4 days
Animal Experiment
Animal models SCID mice (8–10 per group) bearing MDA-MB-231 xenograft model
Formulation saline
Dosages 10,30 and 100 mg/kg 5 days a week for 2 weeks
Administration oral gavage
Chemical Information
Molecular Weight 561.71
Formula C32H43N5O4
CAS Number 1071992-99-8
Solubility (25°C) DMSO 85 mg/mL
Ethanol 85 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Brunckhorst MK, et al. Cancer Biol Ther. AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer.

[2] Cai Q, et al. J Med Chem. A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.

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Keywords: AT-406, SM-406; Xevinapant; Debio 1143 supplier, IAP, inhibitors, activators

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