AZD5582 is a class of dimeric Smac mimetics as potent IAP antagonist and binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
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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 |
+++
cIAP1-BIR3, Ki: 17 nM cIAP2-BIR3, Ki: 43 nM |
++
XIAP-BIR2, Ki: 112 nM XIAP-BIR3, Ki: 28 nM |
99%+ | ||||||||||||||||
Xevinapant |
++++
cIAP1-BIR3, Ki: 1.9 nM cIAP2-BIR3, Ki: 5.1 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 | AZD5582 is an IAP inhibitor with IC50 values of 15nM, 21nM and 15nM for cIAP1, cIAP2 and XIAP (measured by fluoresence polarization assays), respectively. Treatment with AZD5582 caused cIAP1 degradation with IC50 of 0.1nM and cell growth inhibition with GI50<0.06nM in MDA-MB-231 cells. And induction of cell apoptosis could be observed by AZD5582 at subnanomolar concentration. A single intravenous dose of AZD5582 caused dose (0.05-3mg/kg)- and time (4, 6 and 18h)-degradation of cIAP1 and increased cleaved caspase3 in mice bearing MDA-MB-231 xenografts, suggesting the pharmacodynamics of this compound in vivo. Intravenous injection with AZD5582 at dose of 0.1, 0.5 and 3mg/kg, once a week for 2 weeks, dose-dependently inhibited growth inhibition in the MDA-MB-231 xenograft efficacy model[1]. AZD5582 can target cIAP1 to induce TNF-α-induced apoptosis accompanied with a decrease of Mcl-1 protein, a member of the Bcl-2 family, but not that of Bcl-2 and Bcl-xL[2]. |
作用机制 | AZD5582 can bind potently to the BIR3 domains of cIAP1, cIAP2 and XIAP and cause cIAP1 degradation.[1] |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
BT549 cells | Growth inhibition assay | Growth inhibition of human BT549 cells | 24320998 | ||
MDA-MB-231 cells | Growth inhibition assay | 48 h | Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 48 hrs by Alamar Blue assay, GI50=6e-05 μM | 24320998 |
Dose | Mice[1] (i.v.): min = 0.1 mg/kg, max = 3 mg/kg | ||||||||||||||
Administration | i.v. | ||||||||||||||
Pharmacokinetics |
|
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
0.98mL 0.20mL 0.10mL |
4.92mL 0.98mL 0.49mL |
9.85mL 1.97mL 0.98mL |
CAS号 | 1258392-53-8 |
分子式 | C58H78N8O8 |
分子量 | 1015.289 |
别名 | |
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,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(103.42 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 |