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DEBIO 1143

Chemical Structure : DEBIO 1143

CAS No.: 1071992-99-8

DEBIO 1143 (Xevinapant;AT-406;DEBIO1143;SM406;ARRY-334543;D1143)

Catalog No.: PC-35889Not For Human Use, Lab Use Only.

DEBIO 1143 (Xevinapant, AT-406, SM406, ARRY-334543, D1143) is a potent, orally active Smac mimetic that antagonizes cIAP1, cIAP2 and XIAP with Ki of 66.4, 1.9 and 5.1 nM, respectively.

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Biological Activity

DEBIO 1143 (Xevinapant, AT-406, SM406, ARRY-334543, D1143) is a potent, orally active Smac mimetic that antagonizes cIAP1, cIAP2 and XIAP with Ki of 66.4, 1.9 and 5.1 nM, respectively.
DEBIO 1143 effectively antagonizes XIAP BIR3 protein in cell-free functional assays, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines.
DEBIO 1143 effectively induces apoptosis and causes complete inhibition of tumor growth apoptosis in xenograft tumors.

Physicochemical Properties

M.Wt 561.727
Formula C32H43N5O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(5S,8S,10aR)-N-benzhydryl-5-((S)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide

References

1. Cai Q, et al. J Med Chem. 2011 Apr 28;54(8):2714-26.

2. Langdon CG, et al. Oncotarget. 2015 Nov 10;6(35):37410-25.

3. Tao Z, et al. Clin Cancer Res. 2018 Oct 23. doi: 10.1158/1078-0432.

4. Thibault B, et al. Sci Rep. 2018 Dec 14;8(1):17862.

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