货号:A780789 同义名: AT-406;Debio 1143
Xevinapant (AT-406) 是一种有效的口服生物可利用的 Smac 模拟物,作为 IAPs 的拮抗剂,能够抑制 XIAP、cIAP1 和 cIAP2 蛋白,其 Ki 值分别为 66.4、1.9 和 5.1 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50μL*10mM(DMSO) | ¥201随货¥149 | 咨询 | |
10mM*1mL(DMSO) | ¥1232 | 咨询 | |
1mg | ¥286 | 咨询 | |
5mg | ¥630 | 咨询 | |
10mg | ¥1008 | 咨询 | |
25mg | ¥2205 | 咨询 | |
50mg | ¥3591 | 咨询 | |
1g | ¥23064 | 咨询 |
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产品名称 | cIAP ↓ ↑ | XIAP ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
LCL161 | ✔ | 99%+ | |||||||||||||||||
AZD5582 |
+++
cIAP1, IC50: 15 nM cIAP2, IC50: 21 nM |
+++
XIAP, IC50: 15 nM | 99%+ | ||||||||||||||||
Birinapant |
++++
cIAP1, Kd: <1 nM |
++
XIAP, Kd: 45 nM | 98+% | ||||||||||||||||
GDC-0152 |
+++
cIAP2-BIR3, Ki: 43 nM cIAP1-BIR3, Ki: 17 nM |
++
XIAP-BIR3, Ki: 28 nM XIAP-BIR2, Ki: 112 nM | 99%+ | ||||||||||||||||
Xevinapant |
++++
cIAP2-BIR3, Ki: 5.1 nM cIAP1-BIR3, Ki: 1.9 nM |
+
XIAP-BIR3, Ki: 66.4 nM | 99%+ | ||||||||||||||||
Embelin |
+
XIAP, IC50: 4.1 μM | 99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
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. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 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 | |
MDA-MB-231 cells | Cytotoxicity assay | 72 h | Cytotoxicity against human sensitive MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by Alamar Blue assay, EC50=0.019 μM | 26218264 | |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 1071992-99-8 |
分子式 | C32H43N5O4 |
分子量 | 561.715 |
别名 | AT-406;Debio 1143;ARRY-334543;SM-406 |
运输 | 蓝冰 |
存储条件 | 液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
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 |
动物实验配方 | 30% propylene glycol+5% Tween 80+65% water 30 mg/mL suspension |