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CAS No.: 1071992-99-8

Xevinapant Catalog No. CSN15873

Synonyms: AT-406;Debio 1143;SM-406

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.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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

更多
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01265199	Acute Myelogenous Leukemia (AM... more >>L) Collapse <<	Phase 1	Terminated(Study was terminate... more >>d before a MTD was determined for administrative reasons) Collapse <<	-	United States, Illinois ... more >> Univerity of Chicago Chicago, Illinois, United States United States, Michigan University of Michigan Health System Ann Arbor, Michigan, United States United States, Missouri Washington University at St. Louis Siteman Cancer Center St. Louis, Missouri, United States United States, New York Memorial Sloan Kettering Cancer Center New York, New York, United States United States, Pennsylvania Hospital of the University of Pennsylvania Philadelphia, Pennsylvania, United States Temple University at Jeanes Hospital Philadelphia, Pennsylvania, United States Collapse <<
NCT01078649	Cancer Solid ... more >>Tumors Lymphoma Malignancy Collapse <<	Phase 1	Completed	-	United States, Michigan ... more >> University of Michigan Cancer Center Ann Arbor, Michigan, United States, 48109 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7803 mL
- 8.9013 mL
- 17.8026 mL
- 5 mM
- 0.3561 mL
- 1.7803 mL
- 3.5605 mL
- 10 mM
- 0.1780 mL
- 0.8901 mL
- 1.7803 mL

技术信息

CAS号

1071992-99-8

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C32H43N5O4

运输

蓝冰

分子量

561.71

别名

AT-406;Debio 1143;SM-406;ARRY-334543

溶解度

DMSO	97.0 mg/mL (172.7 mM)
Water	Insoluble
Ethanol	97.0 mg/mL (172.7 mM)

动物实验配方

30% propylene glycol+5% Tween 80+65% water

30 mg/mL

suspension

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT01265199	Acute Myelogenous Leukemia (AM... more >>L) Collapse <<	Phase 1	Terminated(Study was terminate... more >>d before a MTD was determined for administrative reasons) Collapse <<	-	United States, Illinois ... more >> Univerity of Chicago Chicago, Illinois, United States United States, Michigan University of Michigan Health System Ann Arbor, Michigan, United States United States, Missouri Washington University at St. Louis Siteman Cancer Center St. Louis, Missouri, United States United States, New York Memorial Sloan Kettering Cancer Center New York, New York, United States United States, Pennsylvania Hospital of the University of Pennsylvania Philadelphia, Pennsylvania, United States Temple University at Jeanes Hospital Philadelphia, Pennsylvania, United States Collapse <<
NCT01078649	Cancer Solid ... more >>Tumors Lymphoma Malignancy Collapse <<	Phase 1	Completed	-	United States, Michigan ... more >> University of Michigan Cancer Center Ann Arbor, Michigan, United States, 48109 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55905 United States, North Carolina Duke University Medical Center Durham, North Carolina, United States, 27710 Collapse <<

Xevinapant Catalog No. CSN15873

靶点选择性

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