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产品总数：60959
| 中文名称 |
Xevinapant hydrochloride
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|---|---|
| 中文别名 |
AT-406 盐酸盐
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| 英文名称 |
Xevinapant hydrochloride
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| 英文别名 |
Benzeneacetamide, 4-chloro-N-[1-[[(cyanoamino)[(2-methyl-3-pyridinyl)imino]methyl]amino]-2,2-dimethylpropyl]-;AT-406;AT-406 HCl;(5S,8S,10aR)-N-(Diphenylmethyl)decahydro-5-[[(2S)-2-(methylamino)-1-oxopropyl]amino]-3-(3-methyl-1-oxobutyl)-6-oxo-pyrrolo[1,2-a][1,5]diazocine-8-carboxamide hydrochloride (1:1);AT406;SM 406;AT 406;(5S,8S,10aR)-N-benzhydryl-5-((S)-2-(methylamino)propanamido)-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide;Debio 1143;N65WC8PXDD;(5S,8S,10aR)-N-(Diphenylmethyl)-5-[(N-methyl-L-alanyl)amino]-3-(3-methylbutanoyl)-6-oxodecahydropyrrolo[1,2-a][1,5]diazocine-8-carboxamide;GTPL7729;Xevinapant;Xevinapant hydrochloride
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| Cas No. |
1071992-57-8
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| 分子式 |
C32H43N5O4
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| 分子量 |
561.71
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| 包装储存 |
-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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| 产品详情 |
Xevinapant (AT-406) hydrochloride 是一种有效的、口服生物可利用的 Smac 模拟物，也是细胞凋亡蛋白 (IAPs) 抑制剂的拮抗剂。Xevinapant hydrochloride 与 XIAP、cIAP1 和 cIAP2 蛋白结合，Ki 分别为 66.4、1.9 和 5.1 nM。Xevinapant hydrochloride 在无细胞功能测定中有效拮抗 XIAP BIR3 蛋白，诱导细胞 cIAP1 蛋白的快速降解，并抑制各种人类癌细胞系中的癌细胞生长。Xevinapant hydrochloride 在诱导异种移植肿瘤细胞凋亡方面非常有效。
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| 生物活性 |
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.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
cIAP1 1.9 nM (Ki) cIAP2 5.1 nM (Ki)
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| 体外研究(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 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. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
-20°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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| ClinicalTrial |
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| 参考文献 |
[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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| 溶解度数据 |
In Vitro: DMSO : 175 mg/mL (292.55 mM; Need ultrasonic)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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