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  • AT-406

    • SM-406;Debio-1143;ARRY-334543
    货号: abs813319
    CAS号: 1071992-99-8
    分子式: C32H43N5O4
    分子量: 561.71
    产品说明书
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    货号-规格 货期 价格 数量
    abs813319-5mg 1-2周 ¥1320.00
    - +
    abs813319-10mg 1-2周 ¥2062.00
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    abs813319-25mg 1-2周 ¥3881.00
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    abs813319-50mg 1-2周 ¥6588.00
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    大包装询价
    产品描述
    描述

    AT-406是一种有效的,拟Smac的IAP(通过E3泛素连接酶起作用的凋亡蛋白抑制剂)拮抗剂,与XIAP-BIR3, cIAP1-BIR3和cIAP2-BIR3结合,Ki为66.4 nM, 1.9 nM和5.1 nM,比作用于Smac AVPI肽亲和力高50到100倍。

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    SM-406;Debio-1143;ARRY-334543
    可溶性/溶解性
    DMSO :93 mg/mL (165.6 mM)

    Ethanol :93 mg/mL (165.6 mM)
    生物活性
    靶点
    cIAP1-BIR3 ,cIAP2-BIR3 ,XIAP-BIR3
    In vitro(体外研究)
    AT-406 is a Smac mimetic and appears to mimic closely the AVPI peptide in both hydrogen bonding and hydrophobic interactions with XIAP, with additional hydrophobic contacts with W323 of XIAP. AT-406 is more sensitive to these IAPs than Smac AVPI peptide with 50-100 fold binding affinities. AT-406 (at 1 μM) completely restores the activity of caspase-9, which is suppressed by 500 nM XIAP BIR3 in a cell-free system. In MDA-MB-231 cell, AT-406 induces rapid cellular cIAP1 degradation and also pulls down the cellular XIAP protein. AT-406 effectively inhibits lots of human cancer cell lines and shows IC50 of 144 and 142 nM in MDA-MB-231 cell and SK-OV-3 ovarian cell, with low toxicity against normal-like human breast epithelial MCF-12F cells and primary human normal prostate epithelial cells. AT-406 induces apoptosis in MDA-MB-231 cell by inducing activation of caspase-3 and cleavage of PARP.
    In vivo(体内研究)
    AT-406 has good pharmacokinetic (PK) properties and oral bioavailability in mice, rats, non-human primates, and dogs. In the MDA-MB-231 xenograft, AT-406 effectively induces cIAP1 degradation and processing of procaspase-8, cleavage of PARP in tumor tissues at 100 mg/kg with well toleration even at 200 mg/kg. AT-406 induces significant tumor growth inhibition with p of 0.0012 at 100 mg/kg.
    参考文献
    参考文献
    AT-406, an orally active antagonist of multiple inhibitor of apoptosis proteins, inhibits progression of human ovarian cancer.
    Brunckhorst MK,et al. Cancer Biol Ther. 2012 Jul;13(9):804-11. PMID:
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