Xevinapant hydrochloride (Synonyms: AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride) |
| カタログ番号GC63290 |
ゼビナパント (AT-406) 塩酸塩は、経口で生物学的に利用可能な強力な Smac ミメティックであり、アポトーシスタンパク質 (IAP) の阻害剤のアンタゴニストです。塩酸ゼビナパントは、XIAP、cIAP1、および cIAP2 タンパク質に、それぞれ 66.4、1.9、および 5.1 nM の Kis で結合します。塩酸ゼビナパントは、無細胞機能アッセイで XIAP BIR3 タンパク質に効果的に拮抗し、細胞の cIAP1 タンパク質の急速な分解を誘導し、さまざまなヒトがん細胞株のがん細胞の増殖を阻害します。塩酸ゼビナパントは、異種移植腫瘍のアポトーシス誘導に非常に効果的です。
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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