Xevinapant hydrochloride (Synonyms: AT-406 hydrochloride; Debio 1143 hydrochloride; SM-406 hydrochloride) |
رقم الكتالوجGC63290 |
Xevinapant (AT-406) هيدروكلوريد هو محاكى Smac قوي ومتوفر بيولوجيًا عن طريق الفم ومضاد لمثبط بروتينات موت الخلايا المبرمج (IAPs)يرتبط Xevinapant hydrochloride ببروتينات XIAP و cIAP1 و cIAP2 مع Kis من 66.4 و 1.9 و 5.1 نانومتر على التواليهيدروكلوريد Xevinapant يعاكس بشكل فعال بروتين XIAP BIR3 في اختبار وظيفي خالٍ من الخلايا ، ويحث على التدهور السريع لبروتين cIAP1 الخلوي ، ويمنع نمو الخلايا السرطانية في مختلف خطوط الخلايا السرطانية البشريةهيدروكلوريد Xevinapant فعال للغاية في تحريض موت الخلايا المبرمج في أورام طعم أجنبي
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Cas No.: 1071992-57-8
Sample solution is provided at 25 µL, 10mM.
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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