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.
|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 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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 10 mg/mL|
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