Xevinapant

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Chemical Structure| 1071992-99-8 同义名 : AT-406; Debio 1143; ARRY-334543; SM-406
CAS号 : 1071992-99-8
货号 : A780789
分子式 : C32H43N5O4
纯度 : 99%+
分子量 : 561.71
MDL号 : MFCD22124467
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(186.93 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • cIAP

    cIAP2-BIR3, Ki:5.1 nM

    cIAP1-BIR3, Ki:1.9 nM

  • XIAP

    XIAP-BIR3, Ki:66.4 nM
描述 AT406 is a potent and orally bioavailable Smac mimetic and an antagonist of the inhibitor of apoptosis proteins (IAPs), AT-406 binds to XIAP, cIAP1, and cIAP2 proteins with K (i) of 66.4, 1.9, and 5.1 nM, respectively.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
EVSA-T cells Cytotoxicity assay 72 h Cytotoxicity against human sensitive EVSA-T cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay, EC50=0.0021 μM 26218264
HEK293 cells Function assay 2 h Antagonist activity at full-length FLAG-tagged XIAP (unknown origin) transfected in HEK293 cells assessed as inhibition of interaction with caspase 9 after 2 hrs by immunoprecipitation assay, EC50=0.034 μM 26218264
human SKOV3 cells Growth inhibition assay 4 days Growth inhibition of human SKOV3 cells after 4 days by WST8 assay, IC50=0.142 μM 21443232
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.90mL

1.78mL

0.89mL

17.80mL

3.56mL

1.78mL
参考文献

[1]Cai Q, Sun H, 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 Apr 28;54(8):2714-26.

[2]Zhen MC, Wang FQ, et al. Identification of mTOR as a primary resistance factor of the IAP antagonist AT406 in hepatocellular carcinoma cells. Oncotarget. 2017 Feb 7;8(6):9466-9475.