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| 5mg |
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| 25mg |
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| 100mg |
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Purity: ≥98%
HMN-214 (HMN 214; HMN214), stilbene derivative, is a potent and orally bioactive prodrug of HMN-176, which alters the cellular spatial orientation of Plk1 (polo-like kinase-1). Poly-like kinase-1 (PLK1) is a serine/threonine kinase that controls important mitotic events. HMN-214 tampers with PLK1's subcellular geolocation. The mean IC50 of HMN-176 was 118 nM, indicating strong cytotoxicity. Furthermore, compared to other agents tested, HMN-176 was more cytotoxic toward drug-resistant phenotypes of tumor cells as indicated by its low resistance indices.
| Targets |
PLK1
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|---|---|
| ln Vitro |
HMN-214 is a prodrug of HMN-176. HMN-176 has a mean IC50 of 118 nM and exhibits strong activities against 22 human tumor cell lines[1]. In HeLa cells, HMN-176 (3-300 nM) dose-dependently suppresses luciferase expression regulated by the MDR1 promoter. Additionally, complex formation on the Y-box is dose-dependently suppressed by HMN-176 (30-3000 nM)[3]. In PC3-PSMA cells, HMN-214 (3.3 μM) increases luciferase expression 11-fold over vehicle control when using the 1,4C-1,4Bis polymer and 37-fold when using PEI. In MB49 cells, HMN-214 (≥ 3.3 μM) dramatically suppresses cell proliferation and causes notable morphological changes in the cells[4].
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| ln Vivo |
HMN-214 (33 mg/kg, p.o.) converts to HMN-176 in rats. The aciatic and tibial nerves' action potential amplitude and conduction velocity are unaffected by HMN-214. In mice, HMN-214 (20 mg/kg, p.o.) shows antitumor activity[1]. HMN-214 (10, 20 mg/kg, p.o.) reduces the expression of MDR1 mRNA in tumor-derived KB and KB-A.1 in nude mice[3].
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| Enzyme Assay |
HMN-214 is a potent and orally active prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
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| Cell Assay |
The density of cells is seeded at 3 × 103–1 × 104 cells/well in a 96-well microplate. The plate is incubated for 72 hours after dilutions of HMN-214 or HMN-176 are added the following day. Following the MTT assay, IC50 values are obtained, which indicate the degree of growth inhibition.
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| Animal Protocol |
Using an agate pestle, progressively add 0.5% methylcellulose 4000 solution to the ground HMN-214 to create a 3 mg/mL suspension. To get suspensions with the right concentration, this is further diluted with methylcellulose 4000 solution. By s.c. transplantation into naked mice, tumor tissue is grown beforehand. The resulting tumors are excised, cut into 8 mm3 cubic fragments, and then surgically transplanted subcutaneously using a trocar into the right axillary region of naked mice. On day 1, oral administration of HMN-214 is initiated once the tumor's theoretical volume has reached approximately 145 mm3.
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| References |
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| Additional Infomation |
N-(4-methoxyphenyl)sulfonyl-N-[2-[2-(1-oxido-4-pyridin-1-iumyl)ethenyl]phenyl]acetamide is a sulfonamide.
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| Molecular Formula |
C22H20N2O5S
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|---|---|---|
| Molecular Weight |
424.47
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| Exact Mass |
424.109
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| Elemental Analysis |
C, 62.25; H, 4.75; N, 6.60; O, 18.85; S, 7.55
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| CAS # |
173529-46-9
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| Related CAS # |
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| PubChem CID |
9888590
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
663.1±65.0 °C at 760 mmHg
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| Flash Point |
354.8±34.3 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.598
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| LogP |
1.85
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
30
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| Complexity |
689
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])[H])(N(C(C([H])([H])[H])=O)C1=C([H])C([H])=C([H])C([H])=C1/C(/[H])=C(\[H])/C1C([H])=C([H])[N+](=C([H])C=1[H])[O-])(=O)=O
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| InChi Key |
OCKHRKSTDPOHEN-BQYQJAHWSA-N
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| InChi Code |
InChI=1S/C22H20N2O5S/c1-17(25)24(30(27,28)21-11-9-20(29-2)10-12-21)22-6-4-3-5-19(22)8-7-18-13-15-23(26)16-14-18/h3-16H,1-2H3/b8-7+
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| Chemical Name |
N-(4-methoxyphenyl)sulfonyl-N-[2-[(E)-2-(1-oxidopyridin-1-ium-4-yl)ethenyl]phenyl]acetamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.62 mg/mL (1.46 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.62 mg/mL (1.46 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.62 mg/mL (1.46 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 0.5% methylcellulose: 30 mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3559 mL | 11.7794 mL | 23.5588 mL | |
| 5 mM | 0.4712 mL | 2.3559 mL | 4.7118 mL | |
| 10 mM | 0.2356 mL | 1.1779 mL | 2.3559 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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