| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| 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].
|
|---|---|
| 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].
|
| 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. |
| 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. |
| References |
| Molecular Formula |
C21H24N2O4
|
|---|---|
| Molecular Weight |
368.426265716553
|
| Exact Mass |
368.173
|
| CAS # |
2237054-53-2
|
| PubChem CID |
137319628
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.8
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
27
|
| Complexity |
430
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(C)C1C(=C(C=C(C=1)C1C(=CN(C)N=1)C1C=CC(=CC=1)OCC)OC)OC
|
| InChi Key |
YWYCRTNRTJCKHS-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
4-(4-ethoxyphenyl)-1-methyl-3-(3,4,5-trimethoxyphenyl)pyrazole
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ≥ 125 mg/mL (~339.28 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
