Hesperadin
目录号: PL02451 纯度: ≥98%
CAS No. :422513-13-1
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中文名称
Hesperadin
中文别名
Hesperadin 抑制剂;N-[(3Z)-2-氧代-3-[苯基-[4-(哌啶-1-甲基)苯胺]亚甲基]-1H-吲哚-5-基]乙烷磺酰胺;N-[2,3-二氢-2-氧代-3-[(3Z)-苯基[[4-(1-哌啶基甲基)苯基]氨基]亚甲基]-1H-吲哚-5-基]乙磺酰胺;(Z)-N-[2-氧代-3-[苯基[[4-(哌啶-1-基甲基)苯基]氨基]亚甲基]吲哚啉-5-基]乙磺酰胺
英文名称
Hesperadin
英文别名
Hesperadin;(2Z)-(2-AMINOTHIAZOL-4-YL)(METHOXYIMINO)ACETIC ACID;Hesperadin hydrochloride;Hesperidin;N-[(3Z)-2-oxo-3-[phenyl-[4-(piperidin-1-ylmethyl)anilino]methylidene]-1H-indol-5-yl]ethanesulfonamide;UNII-PTR491OS14;(Z)-N-[2-Oxo-3-[phenyl[[4-(piperidin-1-ylmethyl)phenyl]amino]methylene]indolin-5-yl]ethanesulfonamide (This product is unavailable in the U.S.);Hesperadine;N-[2,3-Dihydro-2-oxo-3-[(3Z)-phenyl[[4-(1-piperidinylmethyl)phenyl]amino]methylene]-1H-indol-5-yl]ethanesulfonamide;PTR491OS14;AK174795;C29H32N4O3S;(Z)-N-(2-oxo-3-(phenyl(4-(piperidin-1-ylmethyl)phenylamino)methylene)indolin-5-yl)ethanesulfonamide;(Z)-N-(2-oxo-3-(phenyl((4-(piperidin-1-ylmethyl)phenyl)amino)methylene)indolin-5-yl)ethanesulfonamide;N-[(3Z)-2-oxo-3-(phenyl{[4-(piperidin-1-ylmethyl)phenyl]amino;N-{(3Z)-2-oxo-3-[phenyl({4-[(piperidin-1-yl)methyl]phenyl}amino)methylidene]-2,3-dihydro-1H-indol-5-yl}ethanesulfonamide;N-[(3Z)-2-oxo-3-(phenyl{[4-(piperidin-1-ylmethyl)phenyl]amino}methyli
Cas No.
422513-13-1
分子式
C29H32N4O3S
分子量
516.65
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Hesperadin 是 Aurora A 和 B 的 ATP 竞争性吲哚酮抑制剂。Hesperadin 以 250 nM 的 IC50 抑制 Aurora B。Hesperadin 通过阻断核分裂和胞质分裂而抑制布鲁氏锥虫的生长。Hesperadin 也是一种广谱流感抗病毒剂。
生物活性
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC 50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
性状
Solid
IC50 & Target[1][2]
Trypanosoma Aurora B 250 nM (IC50)
体外研究(In Vitro)
Hesperadin (10-100 nM) inhibits the Aurora kinase-1 (TbAUK1)-mediated phosphoryation of trypanosome histone H3 (TbH3) in a dose dependent manner, with an IC50 of 40 nM.
Hesperadin (0.01-10 μM; 24 or 48 hours) inhibits growth of bloodstream forms (BF) and procyclic forms (PF) cultures.
Hesperadin (100-200 nM; 24-72 hours) alters cell morphology and inhibits cell cycle progression similar to the RNAi knockdown of TbAUK1.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Hesperadin (20 mg/kg/d; i.v.) prolongs the survival of xenograft mice via synergistic effect with temozolomide (TMZ). has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-week-old female
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]. Neal J, et, al. The cell cycle as a therapeutic target against Trypanosoma brucei: Hesperadin inhibits Aurora kinase-1 and blocks mitotic progression in bloodstream forms. Mol Microbiol. 2009 Apr; 72(2): 442-58.
[2]. Wahafu A, et, al. Targeting Aurora kinase B attenuates chemoresistance in glioblastoma via a synergistic manner with temozolomide. Pathol Res Pract. 2019 Nov; 215(11): 152617.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (193.55 mM)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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