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| Targets |
The primary target of TN-16 is tubulin. It binds to the colchicine site on tubulin, inhibiting the polymerization of microtubules. TN-16 blocks the assembly and promotes the dissociation of microtubules. By disrupting microtubule dynamics, TN-16 prevents the stabilization of microtubules and blocks the cell cycle in M-phase.
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| ln Vitro |
In vitro, TN-16 is a synthetic inhibitor of microtubule polymerization with an IC50 of 0.4-1.7 μM. It binds to the colchicine site on tubulin and inhibits alkylation of tubulin. TN-16 blocks the assembly and promotes the dissociation of microtubules. It causes metaphase arrest in renal cell carcinoma cells.
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| ln Vivo |
In vivo, TN-16 can be used in combination with other inhibitors to improve the efficiency of artificial chromosome transfer to recipient cells. However, specific in vivo efficacy data from animal models are limited in the available literature.
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| Enzyme Assay |
In vitro enzyme or receptor binding assays for TN-16 involve studying its binding to tubulin. The assay uses purified tubulin and measures the inhibition of microtubule polymerization spectrophotometrically. The compound is incubated with tubulin at varying concentrations to determine the IC50 (0.4-1.7 μM). Competition binding assays with [3H]colchicine can be used to confirm binding to the colchicine site.
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| Cell Assay |
In vitro cell-based assays for TN-16 are performed using various cancer cell lines. Cells are treated with the compound, and cell cycle analysis is performed using flow cytometry. The compound's ability to cause metaphase arrest is assessed. Cell viability and proliferation are measured using standard assays.
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| Animal Protocol |
In vivo animal experiments for TN-16 are limited. The compound can be used in combination with other inhibitors to improve the efficiency of artificial chromosome transfer to recipient cells. However, specific detailed protocols for in vivo studies are not well-documented.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of TN-16 indicate that it has a molecular weight of 306.36 and a molecular formula of C19H18N2O2. The CAS number is 33016-12-5. The IUPAC name is 5-benzyl-3-(1-(phenylamino)ethylidene)pyrrolidine-2,4-dione. It has a melting point of 182-185°C. It is a solid with a purity of ≥95%.
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| Toxicity/Toxicokinetics |
Toxicology (toxicology) data for TN-16 are characteristic of a research compound. As a microtubule polymerization inhibitor, its safety profile is an important consideration. The compound is generally well-tolerated at effective doses in preclinical models. However, its long-term safety profile requires further evaluation.
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| References | |
| Additional Infomation |
Other information: TN-16 is a synthetic inhibitor of microtubule polymerization. It binds to the colchicine site on tubulin. The compound blocks the assembly and promotes the dissociation of microtubules. It is used in research to study microtubule dynamics and cell cycle regulation. Its CAS number is 33016-12-5.
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| Molecular Formula |
C19H18N2O2
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|---|---|
| Molecular Weight |
306.36
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| Exact Mass |
306.137
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| Elemental Analysis |
C, 74.49; H, 5.92; N, 9.14; O, 10.44
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| CAS # |
33016-12-5
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| Related CAS # |
33016-12-5
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| PubChem CID |
135427136
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| Appearance |
White to off-white solid powder
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| Density |
1.249g/cm3
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| Boiling Point |
532.7ºC at 760 mmHg
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| Melting Point |
182-185 °C
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| Flash Point |
195.5ºC
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| Index of Refraction |
1.648
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| LogP |
3.084
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
23
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| Complexity |
498
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C=CC(N/C(=C2/C(=O)NC(CC3C=CC=CC=3)C/2=O)/C)=CC=1
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| InChi Key |
IHXKJZIDPGITHW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H18N2O2/c1-13(20-15-10-6-3-7-11-15)17-18(22)16(21-19(17)23)12-14-8-4-2-5-9-14/h2-11,16,22H,12H2,1H3,(H,21,23)
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| Chemical Name |
2-benzyl-3-hydroxy-4-(C-methyl-N-phenylcarbonimidoyl)-1,2-dihydropyrrol-5-one
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| Synonyms |
TN16 NSC-239274 TN 16 NSC239274 TN-16
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2641 mL | 16.3207 mL | 32.6413 mL | |
| 5 mM | 0.6528 mL | 3.2641 mL | 6.5283 mL | |
| 10 mM | 0.3264 mL | 1.6321 mL | 3.2641 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.
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