TNP-470
Based on 2 publication(s) in Google Scholar
TNP-470 is a methionine aminopeptidase-2 inhibitor and also an angiogenesis inhibitor.
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- Pureté: 99.87%
- CAS No.: 129298-91-5
- Formule: C19H28ClNO6
- Masse moléculaire:401.88
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Stockage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) TNP-470
More
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
5.3 μM
Compound: 3 (TNP-470)
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In vitro antiproliferative effect against A431 human epidermoid carcinoma cells
In vitro antiproliferative effect against A431 human epidermoid carcinoma cells
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10.1016/S0960-894X(96)00564-1 |
| A549 | IC50 |
50 μM
Compound: TNP470
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Antiproliferative activity human A549 cells after 20 hrs by MTT assay
Antiproliferative activity human A549 cells after 20 hrs by MTT assay
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[PMID: 20149494] |
| Bel-7402 | IC50 |
≥50 μM
Compound: TNP470
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Antiproliferative activity human Bel7402 cells after 20 hrs by MTT assay
Antiproliferative activity human Bel7402 cells after 20 hrs by MTT assay
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[PMID: 20149494] |
| BGC-823 | IC50 |
1.48 μM
Compound: TNP-470
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Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay
Antiproliferative activity against human BGC823 cells after 24 hrs by MTT assay
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[PMID: 21925884] |
| CPAE | IC50 |
0.04 ng/mL
Compound: 7
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Tested in vitro for its ability to inhibit cell proliferation of calf pulmonary artery endothelial cells measured calorimetrically by SRB method
Tested in vitro for its ability to inhibit cell proliferation of calf pulmonary artery endothelial cells measured calorimetrically by SRB method
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[PMID: 10636239] |
| EL4 | IC50 |
0.03 ng/mL
Compound: 7
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Tested in vitro for its ability to inhibit cell proliferation of lymphoma EL-4 cells measured calorimetrically by MTT method
Tested in vitro for its ability to inhibit cell proliferation of lymphoma EL-4 cells measured calorimetrically by MTT method
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[PMID: 10636239] |
| HeLa | IC50 |
2.02 μM
Compound: TNP-470
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Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay
Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay
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[PMID: 21925884] |
| HepG2 | IC50 |
0.86 μM
Compound: TNP-470
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Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay
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[PMID: 21925884] |
| HUVEC | IC50 |
0.2 nM
Compound: 2a
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Growth inhibition of HUVEC cells by XTT assay
Growth inhibition of HUVEC cells by XTT assay
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[PMID: 17636946] |
| HUVEC | IC50 |
0.5 μM
Compound: TNP-470
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Antiangiogenic activity against HUVEC assessed as inhibition of VEGF-induced cell migration by NCI antiangiogenesis assay
Antiangiogenic activity against HUVEC assessed as inhibition of VEGF-induced cell migration by NCI antiangiogenesis assay
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[PMID: 19084416] |
| HUVEC | IC50 |
1 μM
Compound: TNP-470
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Antiangiogenic activity against HUVEC assessed as inhibition of capillary-like structure formation by NCI antiangiogenesis assay
Antiangiogenic activity against HUVEC assessed as inhibition of capillary-like structure formation by NCI antiangiogenesis assay
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[PMID: 19084416] |
| HUVEC | IC50 |
3.16 μM
Compound: TNP-470
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Antiangiogenic activity against HUVEC assessed as growth inhibition by NCI antiangiogenesis assay
Antiangiogenic activity against HUVEC assessed as growth inhibition by NCI antiangiogenesis assay
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[PMID: 19084416] |
| HUVEC | IC50 |
0.0089 μM
Compound: TNP470
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Antiproliferative activity HUVEC after 20 hrs by MTT assay
Antiproliferative activity HUVEC after 20 hrs by MTT assay
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[PMID: 20149494] |
| HUVEC | IC50 |
0.76 nM
Compound: TNP470
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Antiproliferative activity against human HUVEC cells after 96 hrs by MTT assay
Antiproliferative activity against human HUVEC cells after 96 hrs by MTT assay
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[PMID: 21296467] |
| HUVEC | IC50 |
1.96 μM
Compound: TNP-470
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Antiproliferative against HUVEC after 48 hrs by MTT assay
Antiproliferative against HUVEC after 48 hrs by MTT assay
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[PMID: 23582273] |
| MCF7 | IC50 |
≥50 μM
Compound: TNP470
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Antiproliferative activity human MCF7 cells after 20 hrs by MTT assay
Antiproliferative activity human MCF7 cells after 20 hrs by MTT assay
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[PMID: 20149494] |
| P388 | IC50 |
>10 ng/mL
Compound: 7
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Tested in vitro for its ability to inhibit cell proliferation of murine leukemia P388D1 cells measured calorimetrically by MTT method
Tested in vitro for its ability to inhibit cell proliferation of murine leukemia P388D1 cells measured calorimetrically by MTT method
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[PMID: 10636239] |
| P388 | IC50 |
>=10 μg/mL
Compound: TNP-470 (3)
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Inhibitory concentration against Murine leukemia P388 measured for endothelial cell proliferation activity
Inhibitory concentration against Murine leukemia P388 measured for endothelial cell proliferation activity
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[PMID: 15978809] |
| SW 1116 | IC50 |
5.54 μM
Compound: TNP-470
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Antiproliferative activity against human SW1116 cells after 24 hrs by MTT assay
Antiproliferative activity against human SW1116 cells after 24 hrs by MTT assay
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[PMID: 21925884] |
No significant difference of apoptotic cell numbers is observed between cells treated with TNP-470 and the controls. The IC50s of TNP-470 are 16.86±0.9 μg/mL, 3.16±0.6 μg/mL and 1.78±0.8 μg/mL for KKU-M213 cells at 24, 48 and 72 h, respectively. The results show that TNP-470 significantly reduces the number of migrated cells and invaded cells as compared with the vehicle treated group. TNP-470 decreases the migrated cells of KKU-M213 to 26% and of KKU-M214 to 11% (P<0.01). Similarly, TNP-470 also significantly affects cell invasion, the number of invaded cells is reduced to 25% in KKU-M213 (P<0.01) and to 15% in KKU-M214 (P<0.01). The relative expressions of MMP2, MMP9 and c-MYC in TNP-470 treated cells are significantly suppressed compared to the vehicle treated cells[1].
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 129298-91-5
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Appearance Solid-Liquid Mixture
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Masse moléculaire 401.88
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Formule C19H28ClNO6
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Color Colorless to off-white
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SMILES
C[C@]1([C@@H](C/C=C(C)/C)O1)[C@]([C@@H]2OC)([H])[C@]3(CC[C@H]2OC(NC(CCl)=O)=O)CO3
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Synonyms
AGM-1470
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Exp Mol Med
Neutrophil extracellular traps mediate the crosstalk between plaque microenvironment and unstable carotid plaque formation. [Abstract]2024 Aug;56(8):1717-1735. PMID: 39085350 -
Solvant et solubilité
DMSO : 100 mg/mL (248.83 mM; Need ultrasonic; 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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (12.44 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (12.44 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
MTT assays are applied to test cell viability. In brief, 3×103 cells per well are seeded in a 96-well plate and incubated with various concentration of TNP-470 for 24, 48, and 72 h at 37°C, 5% CO2. For comparison, cells cultured in the absence of TNP-470 are used as a control. After an incubation period, 10 μL MTT (0.5 mg/mL final concentration) is added to each well. After 4 h of additional incubation, 100 μL of 0.01 N HCl in isopropanol is added to dissolve the crystals. Absorption at 570 nm is determined by ELISA plate reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Individually housed, 4 wk old male C57BL/6 mice are used in this study. After a 1 wk acclimation period, mice are randomly allocated to receive either standard chow diet or high-fat diet for 6.5 wk. Throughout the high-fat feeding period the mice are treated with TNP-470 at a dose of 20 mg/kg body weight, injected subcutaneously every other day (TNP; n=7) or a vehicle injection of an equivalent volume (HFF controls; n=7). Vehicle injections contain 3% ethanol in phosphate-buffered saline. Chow-fed control mice (chow; n=8) are sham injected. Mice are fed ad libitum with food replaced every 2 or 3 days. Body weights are collected three times per week. After 6.5 wk of feeding, animals are fasted for 16-h and sacrificed. Final body, liver, and epididymal adipose tissue weights are measured. Liver and adipose tissue samples are frozen in liquid nitrogen and stored at -80°C for subsequent analysis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kidoikhammouan S, et al. TNP-470, a methionine aminopeptidase-2 inhibitor, inhibits cell proliferation, migration and invasion of human cholangiocarcinoma cells in vitro. Asian Pac J Cancer Prev. 2012;13 Suppl:155-60. [Content Brief]
[2]. White HM, et al. The angiogenic inhibitor TNP-470 decreases caloric intake and weight gain in high-fat fed mice. Obesity (Silver Spring). 2012 Oct;20(10):2003-9. [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, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4883 mL | 12.4415 mL | 24.8830 mL | 62.2076 mL |
| 5 mM | 0.4977 mL | 2.4883 mL | 4.9766 mL | 12.4415 mL | |
| 10 mM | 0.2488 mL | 1.2442 mL | 2.4883 mL | 6.2208 mL | |
| 15 mM | 0.1659 mL | 0.8294 mL | 1.6589 mL | 4.1472 mL | |
| 20 mM | 0.1244 mL | 0.6221 mL | 1.2442 mL | 3.1104 mL | |
| 25 mM | 0.0995 mL | 0.4977 mL | 0.9953 mL | 2.4883 mL | |
| 30 mM | 0.0829 mL | 0.4147 mL | 0.8294 mL | 2.0736 mL | |
| 40 mM | 0.0622 mL | 0.3110 mL | 0.6221 mL | 1.5552 mL | |
| 50 mM | 0.0498 mL | 0.2488 mL | 0.4977 mL | 1.2442 mL | |
| 60 mM | 0.0415 mL | 0.2074 mL | 0.4147 mL | 1.0368 mL | |
| 80 mM | 0.0311 mL | 0.1555 mL | 0.3110 mL | 0.7776 mL | |
| 100 mM | 0.0249 mL | 0.1244 mL | 0.2488 mL | 0.6221 mL |
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