HMN-214

製品コードS1485 バッチS148501

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₂H₂₀N₂O₅S
	分子量	424.47	CAS No.	173529-46-9
Solubility (25°C)*	体外	DMSO	12 mg/mL (28.27 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
in vitro	HMN-214 is an oral prodrug that is rapidly converted to HMN-176. The in vitro data of HMN-214 are scarce. However, HMN-176, active metabolite of HMN-214, shows potent and broad-spectrumanti-tumor activity against various cancer cells, including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, with a mean IC50 value of 118 nM. HMN-176 is also cytotoxic to drug-resistant human and murine cell lines, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with IC50 values ranging from 143 nM–265 nM. In HeLa cells, HMN-176 (3 μM) blocks cell cycle at G2/M phase. ^[1] In Doxorubicin-resistant K2/ARS cells, HMN-176 inhibits cell growth with an IC50 value of 2 μM. HMN-176 (3 μM) down-regulates the expression of the multidrug resistance gene (MDR1), due to the disturbance of NF-Y transcription factor binding to the MDR1 promoter. ^[2] In human RPE1 and CFPAC-1 cells, HMN-176 (2.5 μM) delays satisfaction of the spindle assembly checkpoint. HMN-176 (250 nM–2.5 μM) inhibits meiotic spindle assembly and aster formationin Spisula oocytes. HMN-176 (2.5 μM) also inhibits aster microtubule formation from human centrosomes. These results indicate that the anti-tumor activity of HMN-176 is at least partially via disrupting centrosome-mediated MT assembly during mitosis. ^[3]
in vivo	HMN-214 is an oral pro-drug of HMN-176 with improved oral absorption. HMN-214 (30 mg/kg) triggers no obvious neurotoxicity in mice. In mouse xenograft model of PC-3, A549, and WiDr cells, HMN-214 (10 mg/kg–20 mg/kg) inhibits tumor growth. ^[1] In nude mice model bearing multidrug-resistant KB-A.1 cells, HMN-214 (10 mg/kg–20 mg/kg) significantly suppresses MDR1 mRNA expression. ^[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr cells
	濃度	0–10 μM, dissolved in DMSO
	反応時間	72 hours
	実験の流れ	Cells are seeded into a 96-well microplate at a density of 3 × 10³–1 × 10⁴ cells/well. Dilutions of HMN-214 or HMN-176 are added the next day and the plate is incubated for 72 hours. The inhibition of growth is measured by the MTT assay and IC50 values are then obtained.
動物実験	動物モデル	Male BALB/c nude mice bearing xenografts of PC-3, A549, and WiDr cells
	投薬量	10 mg/kg–20 mg/kg
	投与方法	Oral gavage on a QD × 28 schedule

参考

カスタマーフィードバック

: , , J Control Release, 2015, 204:20-29.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening [ Cancers (Basel), 2022, 14(6)1575]	PubMed: 35326726
Development of a miRNA-controlled dual-sensing system and its application for targeting miR-21 signaling in tumorigenesis [ Exp Mol Med, 2020, 10.1038/s12276-020-00537-z]	PubMed: 33311703
A SMN2 Splicing Modifier Rescues the Disease Phenotypes in an In Vitro Human Spinal Muscular Atrophy Model [ Stem Cells Dev, 2019, 28(7):438-453]	PubMed: 30667343
Targeting PLK1 as a novel chemopreventive approach to eradicate preneoplastic mucosal changes in the head and neck. [ Oncotarget, 2017, 8(58):97928-97940]	PubMed: 29228663
Kinome-level screening identifies inhibition of polo-like kinase-1 (PLK1) as a target for enhancing non-viral transgene expression. [ J Control Release, 2015, 204:20-9]	PubMed: 25681050
Kinome-level screening identifies inhibition of polo-like kinase-1 (PLK1) as a target for enhancing non-viral transgene expression. [Christensen MD, et al. J Control Release, 2015, 204:20-29]

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。