Size | Price | |
---|---|---|
100mg | ||
250mg | ||
500mg | ||
Other Sizes |
ln Vitro |
E7130 inhibits microtubule dynamics and shows antiproliferative activity in cancer cells KPL-4, OSC-19, FaDu and HSC-2 with IC50 values of 0.01-0.1 nM, respectively[1]. E7130 (0.15 nM) inhibits TGF-β-induced myofibroblast transformation by disrupting the formation of microtubule network and inactivating PI3K/AKT/mTOR pathway[1].
|
---|---|
ln Vivo |
E7130 (45-180 μg/kg, i.v.) increases intratumoral microvessel density (MVD), thereby enhancing cetuximab (CTX) delivery to tumors, leading to tumor regression in HSC-2 SCCHN xenograft BALB/c mice[1]. E7130 (45-180 μg/kg, i.v.) reduces α-SMA-positive CAFs, and the E7130-CTX combination modulates the phenotype of fibroblasts in FaDu SCCHN xenograft BALB/c mice[1].
|
Cell Assay |
Immunofluorescence[1]
Cell Types: BJ cells Tested Concentrations: 0.15 nM Incubation Duration: 48 h Experimental Results: Inhibited TGF-β-induced α-SMA expression in BJ cells without growth inhibitory activity. Western Blot Analysis[1] Cell Types: BJ cells Tested Concentrations: 0.15 nM Incubation Duration: 48 h Experimental Results: Decreased levels of pAKT and pS6. |
Animal Protocol |
Animal/Disease Models: FaDu SCCHN xenograft BALB/c mice[1]
Doses: 45-180 μg/kg Route of Administration: i.v. Experimental Results: Reduced the α-SMA-positive CAFs, modulated the phenotypes of the fibroblasts with combination of CTX. Animal/Disease Models: HSC-2 SCCHN xenograft BALB/c mice[1] Doses: 90 μg/kg Route of Administration: i.v. Experimental Results: Increased MVD, inhibited tumor growth. Increased survival rate with combination of CTX. |
References |
Molecular Formula |
C58H83NO17
|
---|---|
Molecular Weight |
1066.28
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
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) |
Typically soluble in DMSO (e.g. 10 mM)
|
---|---|
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 | 0.9378 mL | 4.6892 mL | 9.3784 mL | |
5 mM | 0.1876 mL | 0.9378 mL | 1.8757 mL | |
10 mM | 0.0938 mL | 0.4689 mL | 0.9378 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.