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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
Tubulin inhibitor 11 (Compound 48) (0.03-0.1 μM; 12 hours), stops the cell cycle at the G2/M phase. In cells, tubulin inhibitor 11 phosphorylates histone H3 at Ser10 while increasing cyclin B1 and decreasing cdc2 phosphorylation[1]. Compound 48 (0.03-0.3 μM; 48 hours) induces apoptosis in cancer cells [1]. With an IC50 of 8 nM, tubulin inhibitor 11 (Compound 48) has good antiproliferative effects in DU145 cells[1]. 48; 0.03-0.3 μM) dramatically and dose-dependently lowers the expression levels of α-tubulin and acetyl-α-tubulin[1]. 11 tubulin inhibitors
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ln Vivo |
Tubulin inhibitor 11 (Compound 48; po; once daily; 5–10 mg/kg) exhibits strong anticancer efficacies in vivo[1].
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Cell Assay |
Cell Cycle Analysis[1]
Cell Types: DU145 cells Tested Concentrations: 0.01 μM, 0.03 μM, and 0.1 μM Incubation Duration: 12 hrs (hours) Experimental Results: Caused cell cycle arrest at G2/M phase. Apoptosis Analysis[1] Cell Types: DU145 cells Tested Concentrations: 0.03 μM, 0.1 μM, and 0.3 μM Incubation Duration: 48 hrs (hours) Experimental Results: Induced cancer cell apoptosis. Western Blot Analysis[1] Cell Types: DU145 cells Tested Concentrations: 0.01 μM, 0.03 μM, and 0.1 μM Incubation Duration: 12 hrs (hours) Experimental Results: decreased cdc2 phosphorylation and increased cyclin B1 and phosphorylation of histone H3 at Ser10 in cells. |
Animal Protocol |
Animal/Disease Models: Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells[1]
Doses: 5 mg/kg, 10 mg/kg Route of Administration: po; one time/day Experimental Results: Effectively suppressed tumor growth. |
References |
[1]. Songwen Lin, et al. Optimization of Benzamide Derivatives as Potent and Orally Active Tubulin Inhibitors Targeting the Colchicine Binding Site. J Med Chem. 2022 Dec 22;65(24):16372-16391.
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Molecular Formula |
C22H23N3O3S
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Molecular Weight |
409.50
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CAS # |
2366260-33-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C(NCC1=CC=C(C)N=C1)(=O)C1=CC=C(C)C(NS(C2=CC=C(C)C=C2)(=O)=O)=C1
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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) |
DMSO : 100 mg/mL (244.20 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.11 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4420 mL | 12.2100 mL | 24.4200 mL | |
5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | |
10 mM | 0.2442 mL | 1.2210 mL | 2.4420 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.