Xevinapant hydrochloride (Synonyms: AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride) |
| Catalog No.GC63290 |
제비나판트(AT-406) 염산염은 강력하고 경구로 생체이용 가능한 Smac 모방체이며 세포자멸사 단백질(IAP) 억제제의 길항제입니다. 제비나판트 염산염은 각각 66.4, 1.9, 5.1nM의 Kis로 XIAP, cIAP1, cIAP2 단백질에 결합합니다. 제비나판트 염산염은 무세포 기능 분석에서 XIAP BIR3 단백질을 효과적으로 길항하고, 세포 cIAP1 단백질의 빠른 분해를 유도하고, 다양한 인간 암 세포주에서 암세포 성장을 억제합니다. Xevinapant 염산염은 이종이식 종양에서 세포자멸사 유도에 매우 효과적입니다.
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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