HMN-176

Name: HMN-176
Brand: MedChemExpress
SKU: HY-13647
Rating: 4.5 (1 reviews)

Cat. No.: HY-13647 Purity: 98.84%: FAQs
Data Sheet SDS COA Handling Instructions

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HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1), without significant effect on tubulin polymerization.

For research use only. We do not sell to patients.

HMN-176 Chemical Structure

CAS No. : 173529-10-7

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 47	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Protocol
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References
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Description

HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1), without significant effect on tubulin polymerization.

IC₅₀ & Target

PLK1^[5]

In Vitro

HMN-176 (2.5 μM) greatly increases the duration of mitosis in hTERT-RPE1 and CFPAC-1 Cell lines. The effect of HMN-176 on spindle morphology does not appear to be related to effects on microtubule polymerization. HMN-176 (2.5, 0.25, and 0.025 μM) inhibits aster formation in a concentration dependent manner^[1]. HMN-176 (0.1, 1.0, or 10.0 µg/mL) demonstrates inhibitory effects in multiple tumors, with notable activity seen in breast, nonsmall-cell lung, and ovarian cancer specimens. HMN-176 demonstrates activity towards 63% of the breast (5/8), 67% of the non-small cell lung (4/6), and 57% of the ovarian (4/7) tumor specimens treated with 10.0 µg/mL^[2]. HMN-176 shows potent cytotoxicity, with a mean IC₅₀ value of 118 nM. HMN-176 displays similar cytotoxicity against tumors with various characteristics from different organs^[3]. Treatment with 3 μM HMN-176 suppresses the expression of MDR1 mRNA by 56%. HMN-176 has no significant effect on the residual promoter activity^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

After p.o. of HMN-214 to male rats, the prodrug is not detected in the plasma, while plasma levels of HMN-176 peaks at 2 h and gradually decreases thereafter^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

382.43

Formula

C₂₀H₁₈N₂O₄S

CAS No.

173529-10-7

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(OC)C=C1)(NC2=CC=CC=C2/C=C/C3=CC=N(C=C3)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 30 mg/mL (78.45 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.6149 mL	13.0743 mL	26.1486 mL
5 mM	0.5230 mL	2.6149 mL	5.2297 mL
10 mM	0.2615 mL	1.3074 mL	2.6149 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Volume _(start)

Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.84%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (256 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. DiMaio MA, et al. The small organic compound HMN-176 delays satisfaction of the spindle assembly checkpoint by inhibiting centrosome-dependent microtubule nucleation. Mol Cancer Ther. 2009 Mar;8(3):592-601. [Content Brief]

[2]. Medina-Gundrum L, et al. Investigation of HMN-176 anticancer activity in human tumor specimens in vitro and the effects of HMN-176 on differential gene expression. Invest New Drugs. 2005 Jan;23(1):3-9. [Content Brief]

[3]. Takagi M, et al. In vivo antitumor activity of a novel sulfonamide, HMN-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, HMN-176. Invest New Drugs. 2003 Nov;21(4):387-99. [Content Brief]

[4]. Tanaka H, et al. HMN-176, an active metabolite of the synthetic antitumor agent HMN-214, restores chemosensitivity to multidrug-resistant cells by targeting the transcription factor NF-Y. Cancer Res. 2003 Oct 15;63(20):6942-7. [Content Brief]

[5]. Garland LL, et al. A phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors. Clin Cancer Res. 2006 Sep 1;12(17):5182-9. [Content Brief]

Cell Assay ^[3]	Cells to be tested are seeded into a 96-well microplate at a density of 3 ×10³-1×10⁴ cells/well. Drugs are added the next day and the plate is incubated for 72 h at 37 °C in a humidified incubator (5% CO₂, 95% air). The inhibition of growth is measuredby the MTT assay, and the concentration required to produce 50% inhibition of growth (IC₅₀) calculated by the Scansoft 96 software program. The IC₅₀ values for HMN-176 andreference agents are presented. Briefly, for each compound the mean IC₅₀ value for all cell lines tested is calculated and the difference between the individual IC₅₀ values and the mean IC₅₀ value (log10) displayed by a bar projecting to the right or left of the mean. The resistance index is calculated as (IC₅₀ value for drug-resistant cell line)/(IC₅₀ for parent cell line). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	¹⁴C-HMN-214 and ¹⁴C-HMN176 are p.o. to male SD rats at doses of 33 (equivalent to 30 mg/kg of HMN-176) and 30 mg/kg, respectively. Blood samples are collected at designated times and plasma levels of radioactivity determined with a liquid-scintillation counter. In addition, unlabeled HMN-214 (33 mg/kg) is administered to male rats and plasma concentrations of HMN-214 and HMN-176 are determined by high performance liquid chromatography. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. DiMaio MA, et al. The small organic compound HMN-176 delays satisfaction of the spindle assembly checkpoint by inhibiting centrosome-dependent microtubule nucleation. Mol Cancer Ther. 2009 Mar;8(3):592-601. [Content Brief] [2]. Medina-Gundrum L, et al. Investigation of HMN-176 anticancer activity in human tumor specimens in vitro and the effects of HMN-176 on differential gene expression. Invest New Drugs. 2005 Jan;23(1):3-9. [Content Brief] [3]. Takagi M, et al. In vivo antitumor activity of a novel sulfonamide, HMN-214, against human tumor xenografts in mice and the spectrum of cytotoxicity of its active metabolite, HMN-176. Invest New Drugs. 2003 Nov;21(4):387-99. [Content Brief] [4]. Tanaka H, et al. HMN-176, an active metabolite of the synthetic antitumor agent HMN-214, restores chemosensitivity to multidrug-resistant cells by targeting the transcription factor NF-Y. Cancer Res. 2003 Oct 15;63(20):6942-7. [Content Brief] [5]. Garland LL, et al. A phase I pharmacokinetic study of HMN-214, a novel oral stilbene derivative with polo-like kinase-1-interacting properties, in patients with advanced solid tumors. Clin Cancer Res. 2006 Sep 1;12(17):5182-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.6149 mL	13.0743 mL	26.1486 mL	65.3714 mL
	5 mM	0.5230 mL	2.6149 mL	5.2297 mL	13.0743 mL
	10 mM	0.2615 mL	1.3074 mL	2.6149 mL	6.5371 mL
	15 mM	0.1743 mL	0.8716 mL	1.7432 mL	4.3581 mL
	20 mM	0.1307 mL	0.6537 mL	1.3074 mL	3.2686 mL
	25 mM	0.1046 mL	0.5230 mL	1.0459 mL	2.6149 mL
	30 mM	0.0872 mL	0.4358 mL	0.8716 mL	2.1790 mL
	40 mM	0.0654 mL	0.3269 mL	0.6537 mL	1.6343 mL
	50 mM	0.0523 mL	0.2615 mL	0.5230 mL	1.3074 mL
	60 mM	0.0436 mL	0.2179 mL	0.4358 mL	1.0895 mL

HMN-176 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HMN-176173529-10-7HMN176HMN 176Polo-like Kinase (PLK)Inhibitorinhibitorinhibit

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HMN-176

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Complete Stock Solution Preparation Table

HMN-176 Related Classifications

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