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HMN-214

Catalog No. T2438   CAS 173529-46-9
Synonyms: IVX-214, HMN214

HMN-214 (IVX-214) is a potent PLK1 inhibitor with an average IC50 of 0.12 μM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
HMN-214 Chemical Structure
HMN-214, CAS 173529-46-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 77.00
10 mg In stock $ 126.00
25 mg In stock $ 230.00
50 mg In stock $ 369.00
100 mg In stock $ 531.00
500 mg In stock $ 1,180.00
1 mL * 10 mM (in DMSO) In stock $ 84.00
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Purity: 100%
Purity: 99.28%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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.
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)
Synonyms IVX-214, HMN214
Molecular Weight 424.47
Formula C22H20N2O5S
CAS No. 173529-46-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 12 mg/mL (28.27 mM)

TargetMolReferences and Literature

1. Takagi M, et al. Invest New Drugs, 2003, 21(4), 387-399. 2. Tanaka H, et al. Cancer Res, 2003, 63(20), 6942-6947. 3. DiMaio MA, et al. Mol Cancer Ther, 2009, 8(3), 592-601.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Active Compound Library Anti-Cancer Drug Library Kinase Inhibitor Library Inhibitor Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Clinical Compound Library

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Keywords

HMN-214 173529-46-9 Cell Cycle/Checkpoint PLK IVX 214 IVX-214 HMN 214 HMN214 Polo-like Kinase (PLK) inhibit Inhibitor IVX214 inhibitor

 

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