Home Cell Cycle PLK inhibitor HMN-214

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HMN-214 PLK inhibitor

Cat.No.S1485

HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1.
HMN-214 PLK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 424.47

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Chemical Information, Storage & Stability

Molecular Weight 424.47 Formula

C22H20N2O5S

 Storage (From the date of receipt)
CAS No. 173529-46-9 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC(=O)N(C1=CC=CC=C1C=CC2=CC=[N+](C=C2)[O-])S(=O)(=O)C3=CC=C(C=C3)OC

Solubility

In vitro
Batch:

DMSO : 12 mg/mL (28.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Mechanism of Action

Targets/IC50/Ki
PLK1 [1]
In vitro
HMN-214 is an oral prodrug that is rapidly converted to HMN-176. The in vitro data of this compound are scarce. However, HMN-176, active metabolite of this prodrug, shows potent and broad-spectrumanti-tumor activity against various cancer cells, including HeLa, PC-3, DU-145, MIAPaCa-2, U937, MCF-7, A549, and WiDr, with a mean IC50 value of 118 nM. HMN-176 is also cytotoxic to drug-resistant human and murine cell lines, including P388/CDDP, P388/VCR, K2/CDDP, and K2/VP-16, with IC50 values ranging from 143 nM–265 nM. In HeLa cells, HMN-176 (3 μM) blocks cell cycle at G2/M phase. [1] In Doxorubicin-resistant K2/ARS cells, HMN-176 inhibits cell growth with an IC50 value of 2 μM. HMN-176 (3 μM) down-regulates the expression of the multidrug resistance gene (MDR1), due to the disturbance of NF-Y transcription factor binding to the MDR1 promoter. [2] In human RPE1 and CFPAC-1 cells, HMN-176 (2.5 μM) delays satisfaction of the spindle assembly checkpoint. HMN-176 (250 nM–2.5 μM) inhibits meiotic spindle assembly and aster formationin Spisula oocytes. HMN-176 (2.5 μM) also inhibits aster microtubule formation from human centrosomes. These results indicate that the anti-tumor activity of HMN-176 is at least partially via disrupting centrosome-mediated MT assembly during mitosis. [3]
In vivo
HMN-214 is an oral pro-drug of HMN-176 with improved oral absorption. This compound (30 mg/kg) triggers no obvious neurotoxicity in mice. In mouse xenograft model of PC-3, A549, and WiDr cells, this compound (10 mg/kg–20 mg/kg) inhibits tumor growth. [1] In nude mice model bearing multidrug-resistant KB-A.1 cells, this compound (10 mg/kg–20 mg/kg) significantly suppresses MDR1 mRNA expression. [2]
References

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