AZD 5582 dihydrochloride |
カタログ番号GC50109 |
AZD 5582 二塩酸塩は、BIR3 ドメイン cIAP1、cIAP2、および XIAP にそれぞれ 15、21、および 15 nM の IC50 で結合するアポトーシス タンパク質 (IAP) の阻害剤のアンタゴニストです。 AZD5582 はアポトーシスを誘導します。
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Cas No.: 1883545-51-4
Sample solution is provided at 25 µL, 10mM.
Dimeric Smac mimetic; potent inhibitor of X-linked (XIAP) and cellular (cIAP) inhibitor of apoptosis protein (IC50 values are 15, 15 and 21 nM for XIAP, cIAP1 and cIAP2 respectively). Binds to the BIR3 domain of XIAP to prevent interaction with caspase-9. Causes degradation of cIAP1 and cIAP2 and induces apoptosis in MDA-MB-231 breast cancer cells. Causes tumor regression in MDA-MB-231 xenograft-bearing mice.
Hennessy et al (2013) Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582). J.Med.Chem. 56 9897 PMID:24320998
Average Rating: 5
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