Xevinapant hydrochloride

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 K i s 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 In Vitro Xevinapant (AT-406) hydrochloride potently inhibits cell growth in the MDA-MB-231 breast and SK-OV-3 ovarian cancer cell lines with IC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . Xevinapant hydrochloride evaluated for its pharmacokinetic (PK) properties in mice, rats, non-human primates and dogs . 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 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. Form:Solid IC50& Target:cIAP1 1.9 nM (Ki) cIAP2 5.1 nM (Ki) XIAP 66.4 nM (Ki)

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