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100mg | ||
250mg | ||
500mg | ||
Other Sizes |
Targets |
IC50: 1.09 μM (Tubulin polymerization)[1]
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ln Vitro |
Compound 5f, tubulin polymerization-IN-6, exhibits a wide range of anti-proliferation activity against cancer cell lines at concentrations of 0–20 μM over a 24-hour period [1]. Tubulin polymerization-IN-6 (0-100 nM, 24 h) upregulates the expression of Ac-α-tubulin and DeY-α-tubulin and inhibits the formation of tumor cell colonies [1]. Inhibiting tubulin polymerization, tubulin polymerization-IN-6 (0-5 μM, 1 h) directly binds to the colchicine binding site, competing with colchicine for its binding site[1]. The anti-migration activity of tubulin polymerization-IN-6 (0-250 nM, 24 h) against cancer cells is favorable[1]. Tubulin polymerization-IN-6 (0 -50 nM, 24 h) can prevent HUVEC cells from growing angiogenesis[1]. Tubulin polymerization-IN-6 (0-100 nM, 24 h) dose-dependently increases ROS production in HT29 cells and causes cell cycle arrest by regulating associated proteins. It also induces apoptosis by regulating associated proteins and down-regulating mitochondrial membrane potential[1].
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ln Vivo |
Tubulin polymerization-IN-6 (compound 5f) dose-dependently suppresses tumor growth in HT29 xenograft Balb/c nude mice (IP, 0–10 mg/kg, once every two days, for three weeks)[1]. The pharmacokinetic parameters of tubulin polymerization -IN-6 (SD rats, 10 mg/kg, IV, once) are superior[1]. Tubulin polymerization-IN-6 pharmacokinetic parameters in SD rats[1]. 5.67 MRT (h) 1.92 CL (L/h/kg) 1.76 Tmax (h) 0.14 Cmax (ng/mL) 6.88 Parameters 5f t1/2 (h) 1.73 AUC (μg/L·h)
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Cell Assay |
Cell Proliferation Assay
Cell Types: HT29, MCF-7, HeLa, MDA-MB-231, A549[1] Tested Concentrations: 0-20 μM Incubation Duration: 24 h Experimental Results: Had a broad spectrum of anti-proliferation activity against cancer cell lines (MCF-7, MDA-MB-231, A549, Hela, and HT29), with IC50 values of 0.14 ± 0.03, 0.10 ± 0.00, 0.24 ± 0.03, 0.035 ± 0.002, and 0.023 ± 0.001 μM, respectively; and demonstrated moderate anti-proliferative activity against drug resistant cancer cells (MCF-7/TxR and A549/TxR), with IC50 values of 0.18 ± 0.02 and 0.31 ± 0.08 μM, and DRI (drug-resistant index) of 1.3 and 1.2, respectively. Western Blot Analysis Cell Types: HT29 cells[1] Tested Tested Concentrations: 0, 25, 50, and 100 nM Incubation Duration: 24 h Experimental Results: Up-regulated the expression of Ac-α-tubulin (acetyl-α-tubulin) and DeY-α-tubulin (detyrosinated-α-tubulin); regulated the expressions of the proteins involved in cell cycle such as cdc25c, cdk7 , cyclin B1, and cdc2; down-regulated the level of Bim and up-regulated the levels of Bcl-2, p-Bcl-2, and Bax |
Animal Protocol |
Animal/Disease Models: Immunodeficient Balb/c nude mice (HT29 xenograft, 5 weeks old, 36 mice, six groups)[1]
Doses: 0, 5, 7.5, 10 mg/kg Route of Administration: IP, once every two days, for three weeks Experimental Results: Dose-dependently inhibited the tumor growth, inhibits the tumor weight growth by 75.5% at 10 mg/kg. Animal/Disease Models: SD rats (5weeks old)[1] Doses: 10 mg/kg Route of Administration: IV, once (pharmacokinetic/PK Analysis) Experimental Results: demonstrated the better pharmacokinetic/PK properties, demonstrated an eight-fold half-life and a two-fold AUC improvement. |
References |
[1]. Yan XY, Leng JF, Chen TT, Zhao YJ, Kong LY, Yin Y. Design, synthesis, and biological evaluation of novel diphenylamine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site. Eur J Med Chem. 2022;237:114372.
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Molecular Formula |
C19H21NO7
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Molecular Weight |
375.37
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CAS # |
2768613-52-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6640 mL | 13.3202 mL | 26.6404 mL | |
5 mM | 0.5328 mL | 2.6640 mL | 5.3281 mL | |
10 mM | 0.2664 mL | 1.3320 mL | 2.6640 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.