| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Tubulin inhibitor 1 targets tubulin, specifically binding to the colchicine binding site. By binding to this site, the compound inhibits tubulin polymerization and prevents microtubule formation. Microtubules are essential for cell division and intracellular transport, and their disruption leads to mitotic arrest in the G2/M phase and subsequent apoptosis.
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| ln Vitro |
Tubulin inhibitor 1 (compound 7a3) is a tubulin inhibitor that prevents tubulin polymerization [1]. Strong anti-proliferative activity of tubulin inhibitor 1 has been observed against SK-OV-3, MDA-MB-231, HeLa, A549, CT26, and MCF-7 cells; IC50 values are 16.7 ± 3.0, 31.4 ± 0.7, 32.8 ± 2.9, 67.0 ± 0.8, 58.0 ± 2.4, and 35.4 ± 5.6 nM, in that order [1]. In SK-OV-3 cells, tubulin inhibitor 1 (40, 80, and 160 nM, 48 hours) dramatically stopped cell mitosis in the G2/M phase and triggered apoptosis [1].
In vitro, Tubulin inhibitor 1 (compound 7a3) prevents tubulin polymerization. It shows potent anti-proliferative activity against SK-OV-3, MDA-MB-231, HeLa, A549, CT26, and MCF-7 cells with IC₅0 values of 16.7 +/- 3.0, 31.4 +/- 0.7, 32.8 +/- 2.9, 67.0 +/- 0.8, 58.0 +/- 2.4, and 35.4 +/- 5.6 nM, respectively. In SK-OV-3 cells, the compound (40, 80, and 160 nM, 48 hours) dramatically stopped cell mitosis in the G2/M phase and triggered apoptosis. |
| ln Vivo |
Tubulin Inhibitor 1 (50 mg/kg, i.p., three times every two days for 20–25 days) significantly reduced the number of SK-OV-3 cell-bearing Balb/c nude mice while also being well tolerated. of tumor development [1].
In vivo, Tubulin inhibitor 1 (50 mg/kg, i.p., three times every two days for 20-25 days) significantly reduced tumor growth in Balb/c nude mice bearing SK-OV-3 cells while being well tolerated. The compound dramatically diminished tumor growth without causing significant body weight loss. These results demonstrate its potent antitumor efficacy and favorable tolerability in vivo. |
| Enzyme Assay |
For in vitro binding assays, Tubulin inhibitor 1 can be evaluated using tubulin polymerization assays. The compound is incubated with purified tubulin and GTP at various concentrations. Tubulin polymerization is monitored by measuring the increase in absorbance at 350 nm due to light scattering or by fluorescence using tubulin labeled with a fluorescent probe. IC₅0 values for inhibition of polymerization are determined from dose-response curves.
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| Cell Assay |
Apoptosis analysis [1]
Cell Types: SK-OV-3 Cell Tested Concentrations: 40, 80 and 160 nM Incubation Duration: 48 hrs (hours) Experimental Results: SK-OV-3 cells induced apoptosis after 48 hrs (hours) of treatment. For in vitro cellular experiments, Tubulin inhibitor 1 is tested in cancer cell lines such as SK-OV-3, MDA-MB-231, and HeLa. Cells are cultured in appropriate media and treated with various concentrations of the compound. Cell viability and proliferation are assessed using MTT or CellTiter-Glo assays. Cell cycle analysis is performed by flow cytometry to measure G2/M arrest. Apoptosis is evaluated using Annexin V staining or caspase activity assays. |
| Animal Protocol |
Animal/Disease Models: Sixweeks old Balb/c nude mice (18-20 g), carrying SK-OV-3 cells [1]
Doses: 50 mg/kg Route of Administration: IP, 3 times every two days for 20-25 Experimental Results: The tumor growth of Balb/c nude mice carrying SK-OV-3 cells was Dramatically diminished, but the body weight was not Dramatically diminished. For in vivo animal experiments, Tubulin inhibitor 1 can be administered to tumor-bearing mice via intraperitoneal injection. Xenograft models using SK-OV-3 cells in Balb/c nude mice are commonly used. A typical dosing regimen is 50 mg/kg, i.p., three times every two days for 20-25 days. Tumor volume is measured regularly, and body weight is monitored as an indicator of tolerability. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tubulin inhibitor 1 are not extensively detailed in the public literature. As a small molecule with a molecular weight of 368.43, it may have reasonable bioavailability and tissue distribution. The compound is soluble in DMSO at 125 mg/mL. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies.
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| Toxicity/Toxicokinetics |
Toxicological data for Tubulin inhibitor 1 indicate that it is well-tolerated in vivo at efficacious doses. In xenograft mouse models, the compound significantly reduced tumor growth without causing significant body weight loss. Standard toxicological assessments would include acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity evaluations. As with all research chemicals, appropriate safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
Tubulin inhibitor 1 is a research compound used to study tubulin biology and develop anticancer therapies. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. The compound is a tubulin inhibitor that targets the colchicine binding site and has potent anti-tumor activity.
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| Molecular Formula |
C21H24N2O4
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| Molecular Weight |
368.426265716553
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| Exact Mass |
368.173
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| CAS # |
2237054-53-2
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| PubChem CID |
137319628
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| Appearance |
White to off-white solid powder
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
27
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| Complexity |
430
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(C)C1C(=C(C=C(C=1)C1C(=CN(C)N=1)C1C=CC(=CC=1)OCC)OC)OC
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| InChi Key |
YWYCRTNRTJCKHS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H24N2O4/c1-6-27-16-9-7-14(8-10-16)17-13-23(2)22-20(17)15-11-18(24-3)21(26-5)19(12-15)25-4/h7-13H,6H2,1-5H3
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| Chemical Name |
4-(4-ethoxyphenyl)-1-methyl-3-(3,4,5-trimethoxyphenyl)pyrazole
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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 : ≥ 125 mg/mL (~339.28 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.65 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 20.8 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: ≥ 2.08 mg/mL (5.65 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 20.8 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: ≥ 2.08 mg/mL (5.65 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 | 2.7142 mL | 13.5711 mL | 27.1422 mL | |
| 5 mM | 0.5428 mL | 2.7142 mL | 5.4284 mL | |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7142 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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