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HMN-214

Cat. No. M3293

HMN-214 Structure
Size Price Availability Quantity
5mg USD 130 In stock
10mg USD 220 In stock
50mg USD 720 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

HMN-214 (IVX-214, HMN214) is a potent PLK1 inhibitor an average IC50 of 0.12 μM. HMN-176 is an active metabolite of HMN-214 (IVX-214, HMN214). HMN-214 (IVX-214, HMN214) is an oral stilbene derivative. HMN-176 interferes with PLK1, but does not appear to directly inhibit PLK1. Instead, it alters its spatial distribution, resulting in cell cycle arrest at the G2–M phase, with destruction of the spindle polar bodies followed by DNA fragmentation. In human tumor xenografts, there was a broad spectrum of antitumor activity. The antitumor activity of HMN-214 (IVX-214, HMN214) was equal or superior to that of clinically available agents, including cisplatin, doxorubicin, vincristine, and tegafur-uracil.

Protocol
Cell Experiment
Cell lines HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr cells
Preparation method Seeding cells into a 96-well microplate at a density of 3 × 103–1 × 104 cells/well. Adding dilutions of HMN-214 or HMN-176 the next day and incubating the plate for 72 hours. Using the MTT assay to measure cells and then obtaining IC50 values .
Concentrations 0–10 μM, dissolved in DMSO
Incubation time 72 hours
Animal Experiment
Animal models Male BALB/c nude mice bearing xenografts of PC-3, A549, and WiDr cells
Formulation Dissolved in 0.5% methylcellulose
Dosages 10 mg/kg–20 mg/kg
Administration Oral gavage on a QD ?28 schedule
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 424.47
Formula C22H20N2O5S
CAS Number 173529-46-9
Purity >99%
Solubility DMSO 10 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: HMN-214 supplier, PLK, inhibitors

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