Xevinapant hydrochloride (Synonyms: AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride) |
| Catalog No.GC63290 |
Le chlorhydrate de Xevinapant (AT-406) est un mimétique Smac puissant et biodisponible par voie orale et un antagoniste de l'inhibiteur des protéines d'apoptose (IAP). Le chlorhydrate de Xevinapant se lie aux protéines XIAP, cIAP1 et cIAP2 avec un Kis de 66,4, 1,9 et 5,1 nM, respectivement. Le chlorhydrate de Xevinapant antagonise efficacement la protéine XIAP BIR3 dans un essai fonctionnel acellulaire, induit une dégradation rapide de la protéine cIAP1 cellulaire et inhibe la croissance des cellules cancéreuses dans diverses lignées cellulaires cancéreuses humaines. Le chlorhydrate de Xevinapant est très efficace dans l'induction de l'apoptose dans les tumeurs de xénogreffe.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1071992-57-8
Sample solution is provided at 25 µL, 10mM.
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Xevinapant (AT-406) hydrochloride is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). Xevinapant hydrochloride binds to XIAP, cIAP1, and cIAP2 proteins with Kis of 66.4, 1.9, and 5.1 nM, respectively. Xevinapant hydrochloride effectively antagonizes XIAP BIR3 protein in a cell-free functional assay, induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. Xevinapant hydrochloride is highly effective in induction of apoptosis in xenograft tumors[1][2].
Xevinapant (AT-406) hydrochloride potently inhibits cell growth in the MDA-MB-231 breast and SK-OV-3 ovarian cancer cell lines with IC50=144 nM and 142 nM, respectively.Xevinapant (0-3 μM; 0-48 horus) hydrochloride effectively induces cell death in a time- and dose-dependent manner[1].
Xevinapant (AT-406) hydrochloride is very effective in inhibition of tumor growth in the MDA-MB-231 xenograft model, and has minimal toxicity to animals[1]. Xevinapant hydrochloride evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs[1].
[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.
[2]. Brunckhorst MK, et al. AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer. Cancer Biol Ther. 2012;13(9):804-811.
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