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ln Vitro |
Tubulin polymerization-IN-12 (compound 6) exhibits cytotoxicity with an IC50 value of 29.94 μM against normal human embryonic kidney cells (HEK-293)[1]. When it comes to suppressing cancer cells, the IC50 values of Tubulin polymerization-IN-12 (compound 26) are 1.02 μM (A549), 0.75 μM (HeLa), 10.91 μM (HCT116), and 29.94 μM (HEK293) [2]. With an inhibition rate of 42% at 10 μM, tubulin polymerization-IN-12 (1 μM, 2 μM, 10 μM; 6 h) suppresses tubulin expression in HeLa cells [2]. HeLa cells are arrested in the G2/M phase of the cell cycle by tubulin polymerization-IN-12 (0.75 μM-3 μM; 24 h) [2].
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Cell Assay |
Immunofluorescence[2]
Cell Types: HeLa cells Tested Concentrations: 1 μM, 2 μM Incubation Duration: 6 hrs (hours) Experimental Results: Dose -dependently diminished the level of α and β tubulin. Cell Cycle Analysis[2] Cell Types: HeLa cells Tested Concentrations: 0.75 μM, 1.5 μM, 3 μM Incubation Duration: 24 hrs (hours) Experimental Results: Demonstrated 15.03% (0.75 μM), 20.04% ( 1.50 μM), and 33.47% (3.00 μM) of cell accumulation in G2/M phase. |
References |
[1]. Yang F, et al. Synthesis, and biological evaluation of 3, 6-diaryl-[1, 2, 4] triazolo [4, 3-a] pyridine analogues as new potent tubulin polymerization inhibitors[J]. European Journal of Medicinal Chemistry, 2020, 204: 112625.
[2]. Yang F, et al. Novel [1, 2, 4] triazolo [1, 5-a] pyrimidine derivatives as potent antitubulin agents: Design, multicomponent synthesis and antiproliferative activities[J]. Bioorganic Chemistry, 2019, 92: 103260. |
Molecular Formula |
C23H23N5O6
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Molecular Weight |
465.46
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CAS # |
2377301-45-4
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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 | 2.1484 mL | 10.7421 mL | 21.4841 mL | |
5 mM | 0.4297 mL | 2.1484 mL | 4.2968 mL | |
10 mM | 0.2148 mL | 1.0742 mL | 2.1484 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.