Size : 1mLx10mM(inDMSO)
Synonyms: IVX-214, HMN214
| Description | HMN-214 (IVX-214) is a potent PLK1 inhibitor with an average IC50 of 0.12 μM. |
| Targets & IC50 | PLK1:0.12 μM. |
| In vitro | HMN-214, an oral prodrug of HMN-176, exhibits superior oral bioavailability. In nude mouse models carrying multi-drug resistant KB-A.1 cells, HMN-214 (10 mg/kg-20 mg/kg) significantly inhibits the expression of MDR1 mRNA. Additionally, in mouse xenograft models of PC-3, A549, and WiDr cells, HMN-214 (10 mg/kg-20 mg/kg) effectively suppresses tumor growth. |
| In vivo | HMN-214 is an orally administered prodrug that quickly converts to HMN-176, with limited in vitro data available. The active metabolite, HMN-176, demonstrates effective and broad-spectrum antitumor activity against a variety of cancer cell lines including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, with an average IC50 value of 118 nM. HMN-176 at concentrations ranging from 250 nM to 2.5 μM inhibits mitotic spindle assembly and at 2.5 μM also impedes microtubule formation from the centrosome. These outcomes suggest that HMN-176's anticancer activity is, in part, mediated by disrupting centrosome-driven microtubule (MT) assembly during mitosis. Additionally, at 2.5 μM, HMN-176 delays the formation of the proper spindle assembly checkpoint in human RPE1 and CFPAC-1 cells. By disrupting the interaction between the NF-Y transcription factor and the MDR1 promoter, HMN-176 (3 μM) downregulates the expression of the multidrug resistance gene (MDR1). In HeLa cells, HMN-176 (3 μM) blocks cell cycle progression at the G2/M phase. HMN-176 also exhibits cytotoxic effects on both human and murine cell lines resistant to various treatments, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with IC50 values ranging from 143 nM to 265 nM. |
| Synonyms | IVX-214, HMN214 |
| Cell Research | 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.(Only for Reference) |
| Molecular Weight | 424.47 |
| Formula | C22H20N2O5S |
| Cas No. | 173529-46-9 |
| Smiles | N(S(=O)(=O)C1=CC=C(OC)C=C1)(C(C)=O)C2=C(/C=C/C=3C=CN(=O)=CC3)C=CC=C2 |
| Relative Density. | 1.24 g/cm3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 16.7 mg/mL (39.34 mM), Sonication is recommended.  | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Saline: < 1.67 mg/mL (3.93 mM), Lower concentrations may be soluble, but exact solubility limit is unknown. 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1.67 mg/mL (3.93 mM), Solution. 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 0.5 mg/mL (1.18 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
