HMN-176
Based on 1 Customer Validation
HMN-176 is a stilbene derivative which inhibits mitosis, interfering with polo-like kinase-1 (plk1), without significant effect on tubulin polymerization.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.36%
- CAS. Nr.: 173529-10-7
- Formel: C20H18N2O4S
- Molecular Weight:382.43
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
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Biologische Aktivität
PLK1[5]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 173529-10-7
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Appearance Solid
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Molecular Weight 382.43
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Formel C20H18N2O4S
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Color Off-white to light yellow
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SMILES
O=S(C1=CC=C(OC)C=C1)(NC2=CC=CC=C2/C=C/C3=CC=[N+]([O-])C=C3)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
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)
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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
Verweise
[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
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.
| 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
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