DC Chemicals Limited
China
Product Name: HMN-214
Price: $680.0/100mg $1100.0/250mg $2200.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

173529-46-9

173529-46-9 structure

173529-46-9 structure

Name: HMN-214
Chemical Name: N-(4-methoxyphenyl)sulfonyl-N-[2-[(E)-2-(1-oxidopyridin-1-ium-4-yl)ethenyl]phenyl]acetamide
CAS Number: 173529-46-9
Molecular Formula: C₂₂H₂₀N₂O₅S
Molecular Weight: 424.470
Catalog: Biochemical Inhibitor Cell Cycle PLK inhibitor
Create Date: 2016-02-19 10:02:32
Modify Date: 2024-01-02 11:09:57
HMN-214, an orally bioavailable prodrug of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.

Name	N-(4-methoxyphenyl)sulfonyl-N-[2-[(E)-2-(1-oxidopyridin-1-ium-4-yl)ethenyl]phenyl]acetamide
Synonyms	Acetamide, N-[(4-methoxyphenyl)sulfonyl]-N-[2-[(E)-2-(1-oxido-4-pyridinyl)ethenyl]phenyl]- N-[(4-Methoxyphenyl)sulfonyl]-N-{2-[(E)-2-(1-oxido-4-pyridinyl)vinyl]phenyl}acetamide IVX-214 HMN-214 (E)-4-(2-(2-(N-Acetyl-N-((p-methoxyphenyl)sulfonyl)amino)phenyl)ethenyl)pyridine 1-oxide cc-31 Acetamide,N-((4-methoxyphenyl)sulfonyl)-N-(2-((1E)-2-(1-oxido-4-pyridinyl)ethenyl)phenyl) Acetamide,N-((4-methoxyphenyl)sulfonyl)-N-(2-(2-(1-oxido-4-pyridinyl)ethenyl)phenyl)-,(E)

Description	HMN-214, an orally bioavailable prodrug of HMN-176, is an inhibitor of polo-like kinase-1 (plk1), with antitumor activity.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Polo-like Kinase (PLK) Research Areas >> Cancer
Target	PLK1
In Vitro	HMN-214 is a prodrug of HMN-176. HMN-176 shows potent activities against 22 human tumor cell lines, with a mean IC50s of 118 nM[1]. HMN-176 (3-300 nM) inhibits luciferase expression driven by the MDR1 promoter in a dose dependent manner in HeLa cells. HMN-176 (30-3000 nM) also dose-dependently suppresses complex formation on the Y-box[3]. HMN-214 (3.3 μM) enhances luciferase expression relative to vehicle control with the 1,4C-1,4Bis polymer (11-fold) and PEI (37-fold) in PC3-PSMA cells. HMN-214 (≥ 3.3 μM) significantly reduces cell proliferation, causes considerable changes in cell morphology in MB49 cells[4].
In Vivo	HMN-214 (33 mg/kg, p.o.) converts to HMN-176 in rats. HMN-214 has no effect on the conduction velocity and the amplitude of action potentials in the aciatic and tibial nerves. HMN-214 (20 mg/kg, p.o.) exhibits antitumor activity in mice[1]. HMN-214 (10, 20 mg/kg, p.o.) decreases MDR1 mRNA expression in nude mice bearing KB- and KB-A.1.-derived tumors[3].
Cell Assay	Cell proliferation in case of different treatment conditions, relative to untreated control cells (treated as 100% viable, or a live control), is quantified using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT), a yellow colored reagent which is converted to formazan (a purple dye) by living cells. For screening experiments, transfections are carried out in 96-well cell culture plates, that are seeded with 50,000 cells per well. Following 48 h of transfection, 10 μL of MTT reagent is added to the cells and incubated at 37°C for 2-4 h, and the cells are then lysed by adding 20 μL of MTT detergent and incubated for an additional 2 h at room temperature. Inhibitor dose-optimization transfections are carried out in 24-well plates that are seeded with 50,000 cells per well. After 48 h, 20 μL MTT reagent is added, followed by 100 μL of MTT detergent for lysis for 2 h[4].
Animal Admin	The ground HMN-214 is suspended with an agate pestle by gradually adding 0.5% methylcellulose 4000 solution to make a 3 mg/mL suspension. This is additionally diluted with methylcellulose 4000 solution to obtain suspensions of the appropriate concentration. Tumor tissue is grown in advance by s.c. transplantation into nude mice. The resulting tumors are removed, cut into cubic fragments of 8 mm3, and transplanted s.c. into the right axillary region of nude mice with a trocar. When the theoretical volume of the tumor had reached about 145 mm3, oral administration of HMN-214 is started (day 1)[3].
References	[1]. Takagi M, 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]. Garland LL, et al. A phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors. Clin Cancer Res. 2006 Sep 1;12(17):5182-9. [3]. Tanaka H, 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. [4]. Christensen MD, et al. Kinome-level screening identifies inhibition of polo-like kinase-1 (PLK1) as a target for enhancing non-viral transgene expression. J Control Release. 2015 Apr 28;204:20-9.

Density	1.2±0.1 g/cm3
Boiling Point	663.1±65.0 °C at 760 mmHg
Molecular Formula	C₂₂H₂₀N₂O₅S
Molecular Weight	424.470
Flash Point	354.8±34.3 °C
Exact Mass	424.109283
PSA	97.52000
LogP	1.85
Vapour Pressure	0.0±2.0 mmHg at 25°C
Index of Refraction	1.598
Storage condition	-20°C