AZ82
目录号: PL14221 纯度: ≥99%
CAS No. :1449578-65-7
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中文名称
AZ82
英文名称
AZ82
英文别名
AZ82;5-Methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[6-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]propan-2-yl]-4-propylthiophene-2-carboxamide;AOB4872;AZ 82;ZHC57865;BDBM50037967;(2R)-N-[(R)-3-Pyrrolidinyl]-2-[[(4-propyl-5-methyl-2-thienyl)carbonyl]amino]-3-[2-[3-(trifluoromethoxy)phenyl]pyridine-5-yl]propanamide
Cas No.
1449578-65-7
分子式
C28H31F3N4O3S
分子量
560.63
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
AZ82 是一种驱动蛋白样蛋白 KIFC1 (HSET/KIFC1) 的选择性抑制剂,其 Ki 值和 IC50 值分别为 43 nM 和 300 nM。
生物活性
AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a K i of 43 nM and an IC 50 of 300 nM for KIFC1.
性状
Solid
IC50 & Target[1][2]
HSET/KIFC1 300 nM (IC50) HSET/KIFC1 43 nM
体外研究(In Vitro)
AZ82 is shown to specifically induce multipolar spindles in BT-549 cells, but not in cancer cells with normal centrosome number, such as HeLa. AZ82 binds specifically to KIFC1/MT complex but not to KIFC1 or MT alone. Treatment with AZ82 caused centrosome declustering in BT-549 breast cancer cells with amplified centrosomes. AZ82 inhibits both processes with an IC50 of 0.90 ± 0.09 μM for mant-ATP binding and 1.26 ± 0.51 μM for mant-ADP releasing. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Godinho SA, et al. Causes and consequences of centrosome abnormalities in cancer. Philos Trans R Soc Lond B Biol Sci. 2014 Sep 5;369(1650).
[2]. Discovery and mechanistic study of a small molecule inhibitor for motor protein KIFC1. Wu J, et al. ACS Chem Biol. 2013 Oct 18;8(10):2201-8.
溶解度数据
In Vitro: DMSO : 125 mg/mL (222.96 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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