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HMN-214

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Chemical Structure| 173529-46-9 同义名 : IVX-214
CAS号 : 173529-46-9
货号 : A136004
分子式 : C22H20N2O5S
纯度 : 99%+
分子量 : 424.47
MDL号 : MFCD12756255
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 7 mg/mL(16.49 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：

0.5% methylcellulose+water 30 mg/mL suspension

生物活性
靶点

  • PLK1
描述 Polo-like kinase 1 (PLK1), a highly conserved member of the polo-like kinase family, functions specifically during mitosis as a regulator of cell division. PLK1 is spatially and temporally enriched at three distinct subcellular locales: the mitotic centrosomes, kinetochores, and the cytokinetic midbody [3]. HMN-214, an oral prodrug of HMN-176, is an inhibitor of PLK1 through altering its cellular spatial localization. The Cmax and AUC of radioactivity after p.o. of 14C-HMN-214 were 17 and 13 times greater, respectively, than those observed after administration of 14C-HMN-176, demonstrating markedly improved oral absorption of HMN-214 compared with HMN-176. In mice bearing WiDr tumors, HMN-214 exhibited a significant antitumor effect with an IR (inhibitory ratios) value of 73.0% at the MTD (maximum tolerated dose) of 20 mg/kg with a loss in body weight of only 2.7 g. In mice bearing PC-3 tumors, HMN-214 was found to be highly active at the MTD of 20 mg/kg, with an IR value of 78.8%. Moreover, the IR value of HMN-214 was 75.2% at 20 mg/kg in mice bearing A549 tumors [4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.78mL

2.36mL

1.18mL

23.56mL

4.71mL

2.36mL
参考文献

[1]Takagi M, Honmura T, et al. In vivo antitumor activity of a novel sulfonamide, HMN-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, HMN-176. Invest New Drugs. 2003 Nov;21(4):387-99.

[2]Tanaka H, Ohshima N, et al. HMN-176, an active metabolite of the synthetic antitumor agent HMN-214, restores chemosensitivity to multidrug-resistant cells by targeting the transcription factor NF-Y. Cancer Res. 2003 Oct 15;63(20):6942-7.

[3]Colicino EG, Hehnly H. Regulating a key mitotic regulator, polo-like kinase 1 (PLK1). Cytoskeleton (Hoboken). 2018 Nov;75(11):481-494. doi: 10.1002/cm.21504. Epub 2018 Dec 7. PMID: 30414309; PMCID: PMC7113694.

[4]Takagi M, Honmura T, Watanabe S, Yamaguchi R, Nogawa M, Nishimura I, Katoh F, Matsuda M, Hidaka H. In vivo antitumor activity of a novel sulfonamide, HMN-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, HMN-176. Invest New Drugs. 2003 Nov;21(4):387-99. doi: 10.1023/a:1026282716250. PMID: 14586206.