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ln Vitro |
Compound 10, also known as tubulin inhibitor 36, exhibits anti-proliferative effect against human tumor cell lines. The IC50 values are 0.039, 0.038, 0.022, 0.025, and 0.037 against HeLa, MCF7, U87 MG, T98G, HepG2, HCT8, and HT-29 cells, in that order. ,0.040,0.059 micrometers [1]. In HeLa, MCF7, and U87 MG cells, tubulin inhibitor 36 (Compound 10) (100 nM, 24 h, 48 h, and 72 h) can impede mitosis and cause apoptosis [1].
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Cell Assay |
Immunofluorescence[1]
Cell Types: HeLa, MCF7, U87 MG cells Tested Concentrations: 100 nM Incubation Duration: 24 h Experimental Results: Arrested tubulin polymerization in HeLa, MCF7, and U87 MG cells. Cell Cycle Analysis[1] Cell Types: HeLa, MCF7, U87 MG cells Tested Concentrations: 100 nM Incubation Duration: 24 h, 48 h, 72 h Experimental Results: Induced remarkable mitotic arrest in 24 h of HeLa cells. Induced mitotic arrest in 24 h of MCF7 cells but lower cell death compared to HeLa cells Induced remarkable mitotic arrest in 24 h of U87 MG cells and severe cell death. Apoptosis Analysis[1] Cell Types: HeLa, MCF7, U87 MG cells Tested Concentrations: 100 nM Incubation Duration: 72 h Experimental Results: Induced nearly 73% of apoptosis in 72 h of HeLa cells and lower levels of MCF7 cells Induced lower cell death levels of MCF7 cells Displayed the highest cell death levels of d U87 MG cells |
References |
[1]. Gallego-Yerga L, et al. Novel Tetrazole Derivatives Targeting Tubulin Endowed with Antiproliferative Activity against Glioblastoma Cells. Int J Mol Sci. 2023 Jul 4;24(13):11093.
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Molecular Formula |
C16H13CLN6S
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Molecular Weight |
356.83
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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 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.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8025 mL | 14.0123 mL | 28.0245 mL | |
5 mM | 0.5605 mL | 2.8025 mL | 5.6049 mL | |
10 mM | 0.2802 mL | 1.4012 mL | 2.8025 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.