Description
AT-406(SM-406) can inhibit XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM.
Storage
2 years at -20 centigrade
Targets
XIAP, cIAP1, cIAP2
Molecular Formula
C32H43N5O4
Chemical Name
(5S,8S,10aR)-N-benzhydryl-5-((S)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxo-decahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide
Solubility
DSMO 112 mg/mL Water
In vitro
AT-406(SM-406) is a novel, potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs). AT-406(SM-406) can inhibit XIAP, cIAP1, and cIAP2 proteins with Ki of 66.4, 1.9, and 5.1 nM. AT-406(SM-406) can induces rapid degradation of cellular cIAP1 protein, and inhibits cancer cell growth in various human cancer cell lines. In ovarian cancer cells, AT-406(SM-406) shows therapeutic efficacy and mechanism of action in 60% of human ovarian cancer cell lines. 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.
In vivo
In vivo, AT-406(SM-406) inhibits ovarian cancer progression and shows therapeutic potential for patients with inherent or acquired platinum resistance.In the combination with carboplatin, AT-406(SM-406) shows therapeutic efficacy.In vivo, AT-406(SM-406) enhances the carboplatin-induced ovarian cancer cell death and increases survival of the experimental mice by making ovarian cancer cells more sensitive to carboplatin.
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