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| ln Vitro |
There was no discernible variation in the quantity of cells in Qatar between the TNP-470-treated cells and the control group. TNP-470's IC50 values against KKU-M213 cells were 16.86±0.9 μg/mL, 3.16±0.6 μg/mL, and 1.78±0.8 μg/mL at 24, 48, and 72 hours, respectively. The findings demonstrated that TNP -470 dramatically decreased the number of migrating and invading cells as compared to the vehicle-treated group. Migrating cells were decreased by TNP-470 to 26% for KKU-M213 and to 11% for KKU-M214 (P<0.01). The inside of cells was also greatly impacted by TNP-470, with minimum cell counts decreasing to 25% in KKU-M213 (P<0.01) and 15% in KKU-M214 (P<0.01). When compared to cells treated with vehicle, the relative expression of MMP2, MMP9, and c-MYC was markedly suppressed in TNP-470-treated cells [1].
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| ln Vivo |
Even though the TNP-470 model was given a high-fat diet, treatment with TNP-470 reduced (P<0.05) tray accumulation when compared to high-fat feeding (HFF). On day 5, the TNP-470 treatment consumed significantly fewer grams of high-fat food than the catheter-based HFF model. By day 15, treatment with TNP-470 increased (P<0.05) adipose tissue LPL mRNA expression when compared to chow-fed and high-fat-fed pairs. TNP-470 decreases energy admission and increases energy expenditure [2].
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| References |
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| Additional Infomation |
O-(chloroacetylcarbamoyl)fumagiol is a carbamate formed by the conversion of the fumaryl hydroxyl group to the corresponding N-(chloroacetyl)carbamate derivative. It possesses various activities, including methionine aminopeptidase 2 inhibitor, retinoic acid receptor α antagonist, angiogenesis inhibitor, antitumor drug, and EC 1.5.1.3 (dihydrofolate reductase) inhibitor. It is a carbamate, sesquiterpene, organochlorine compound, semi-synthetic derivative, and spirocyclic oxide. Its function is associated with a fumaryl group of compounds. O-(chloroacetylcarbamoyl)fumagiol (TNP-470) has been used in clinical trials investigating the treatment of HIV infection, sarcoma, Kaposi's sarcoma, and pancreatic tumors. O-(chloroacetylcarbamoyl)fumagiol has been reported to exist in Aspergillus fumigatus and Asimina triloba, with relevant data available.
O-Chloroacetylcarbamoylfumagiol is a synthetic analog of fumaril, an antibiotic with antitumor activity isolated from Aspergillus fumigatus fresenius. TNP-470 binds to and irreversibly inactivates methionine aminopeptidase-2 (MetAP2), causing endothelial cell cycle arrest at late G1 phase, thereby inhibiting tumor angiogenesis. This drug may also induce the p53 pathway, thereby stimulating the production of the cyclin-dependent kinase inhibitor p21 and inhibiting angiogenesis. (NCI04) A semi-synthetic analog of aflatoxin, a cyclohexane sesquiterpene antibiotic isolated from Aspergillus fumigatus, which inhibits angiogenesis. |
| Molecular Formula |
C19H28CLNO6
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|---|---|
| Molecular Weight |
401.884
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| Exact Mass |
401.16
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| CAS # |
129298-91-5
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| PubChem CID |
369976
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.535
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| LogP |
1.45
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
636
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(=CC[C@@H]1[C@@](O1)(C)[C@H]2[C@@H]([C@@H](CC[C@]23CO3)OC(=O)NC(=O)CCl)OC)C
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| InChi Key |
MSHZHSPISPJWHW-PVDLLORBSA-N
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| InChi Code |
InChI=1S/C19H28ClNO6/c1-11(2)5-6-13-18(3,27-13)16-15(24-4)12(7-8-19(16)10-25-19)26-17(23)21-14(22)9-20/h5,12-13,15-16H,6-10H2,1-4H3,(H,21,22,23)/t12-,13-,15-,16-,18+,19+/m1/s1
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| Chemical Name |
[(3R,4S,5S,6R)-5-methoxy-4-[(2R,3R)-2-methyl-3-(3-methylbut-2-enyl)oxiran-2-yl]-1-oxaspiro[2.5]octan-6-yl] N-(2-chloroacetyl)carbamate
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| Synonyms |
TNP-470 TNP470 TNP 470 AGM 1470 AGM1470 AGM-1470
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~248.83 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.22 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4883 mL | 12.4415 mL | 24.8830 mL | |
| 5 mM | 0.4977 mL | 2.4883 mL | 4.9766 mL | |
| 10 mM | 0.2488 mL | 1.2442 mL | 2.4883 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00038701 | TERMINATED | Drug: TNP-470 | Pancreatic Neoplasms | M.D. Anderson Cancer Center | 1999-08 | Phase 2 |
| NCT00000763 | COMPLETED | Drug: TNP-470 | HIV Infections Sarcoma, Kaposi |
National Institute of Allergy and Infectious Diseases (NIAID) | 1997-02 | Phase 1 |
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