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| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
Tubulin polymerization-IN-11 (compound 7i) exhibits anti-proliferative activity against HeLa, HEK-293, A549, MCF-7, and T47D cells, with IC50 values of 0.012 and >100, respectively, over a 48-hour period. 10.40, 40.40, 27.91 µM, and 10.40 µM[1]. In the G2/M phase, tubulin polymerization-IN-11 (12, 24, 48 nM; 24 h) dose-dependently causes cellular inflammation and cell cycle events [1]. Polymerization of tubulin-IN-11 (12, 24, 24 h)
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| Cell Assay |
cell proliferation analysis [1]
Cell Types: HeLa, HEK- 48 nM; 24 h) reduces cyclin B1, p-cdc2, Bcl in a dose-based manner -2 protein levels and increase the expression of cleaved PARP protein [1]. 293, A549, MCF-7, T47D Cell Tested Concentrations: 0-100 µM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated anti-proliferative activity against HeLa, HEK-293, A549, MCF, IC50 was 0.012, >100, 10.40, 40.40, 27.91 µM -7, T47D cells, respectively. Cell cycle analysis [1] Cell Types: HeLa Cell Tested Concentrations: 12, 24, 48 nM Incubation Duration: 24 h Experimental Results: Induced cell cycle arrest in G2/M phase, cell percentages were 13.90%, 26.00% and 92.65% respectively. 12, 24, 48 nM. Western Blot Analysis[1] Cell Types: HeLa Cell Tested Concentrations: 12, 24, 48 nM Incubation Duration: 24 hrs (hours) Experimental Results: Concentration-dependent reduction in cyclin B1 and p-cdc2 protein levels. Apoptosis analysis [1] Cell Types: HeLa Cell Tested Concentrations: 12, 24, 48 nM Incubation Duration: 24 h Experimental Results: Induced apoptosis with the total numbers of early and late apoptotic cells were 8.44%, 26.87% and 53.3% at 12, 24, and 48 nM, respectively. |
| 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. Eur J Med Chem. 2020 Oct 15;204:112625.
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| Molecular Formula |
C22H22N4O4
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|---|---|
| Molecular Weight |
406.43
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| Exact Mass |
406.1641052
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| CAS # |
2470063-59-1
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| Related CAS # |
2470063-59-1
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| SMILES |
COC1=C(C=C(C=C1)C2=CN3C(=NN=C3C4=CC(=C(C(=C4)OC)OC)OC)C=C2)N
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| InChi Key |
UHDXUJRRMFTWMJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22N4O4/c1-27-17-7-5-13(9-16(17)23)14-6-8-20-24-25-22(26(20)12-14)15-10-18(28-2)21(30-4)19(11-15)29-3/h5-12H,23H2,1-4H3
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| Chemical Name |
2-methoxy-5-[3-(3,4,5-trimethoxyphenyl)-[1,2,4]triazolo[4,3-a]pyridin-6-yl]aniline
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| Synonyms |
Tubulin polymerization-IN-11
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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 | 2.4604 mL | 12.3022 mL | 24.6045 mL | |
| 5 mM | 0.4921 mL | 2.4604 mL | 4.9209 mL | |
| 10 mM | 0.2460 mL | 1.2302 mL | 2.4604 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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