| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
In BxPC3 pancreatic cancer cells, tigefrin (0.025–10 μM; 20 min) efficiently opposes EphA2 degradation[1]. Targefrin (2–10 μM; 24 h) dramatically reduces the migration of BxPC3 pancreatic cancer cells[1].
|
|---|---|
| ln Vivo |
Combining tartefrin (50 mg/kg; intravenously; for 5 days) with paclitaxel inhibits the growth of tumors[1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: BxPC3 cells(starved for 1 h and pre-treated with Targefrin for 20 min, followed by a combination treatment with 2 μg/mL ephrinA1-Fc for 3 h) Tested Concentrations: 0.025, 0.25, 0.5, 1, 2.5, 5, 7.5 and 10 μM Incubation Duration: 20 min Experimental Results: Effectively antagonized EphA2 induced degradation by the potent ephrinA1-Fc ligand, with an approximate EC50 of ~1.6 μM. Cell Migration Assay [1] Cell Types: BxPC3 cells Tested Concentrations: 2, 4, 5 and 10 μM Incubation Duration: 24 h Experimental Results: Dramatically inhibited pancreatic cancer cell migration. |
| Animal Protocol |
Animal/Disease Models: Male nu/nu (nude) mice (injected with MIA PaCa-2 cells)[1]
Doses: 50 mg/kg Route of Administration: iv; at day 1, 4, 8, 11 and 15 Experimental Results: Both Targefrin-Paclitaxel and Targefrin-dimer-Paclitaxel displayed a significant antitumor effect compared to both the untreated group and the Paclitaxel-treated group. Animal/Disease Models: Balb/ C mice[1] Doses: 50 mg/kg Route of Administration: IV via tail vein; single dosage Experimental Results: Cmax ~650 ng/mL after 2 hrs (hours) from the injection; estimated t1/2 ~15 hr. |
| References |
| Molecular Formula |
C85H116F3N19O15
|
|---|---|
| Molecular Weight |
1700.94
|
| CAS # |
3031514-44-7
|
| Appearance |
White to off-white solid powder
|
| 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) |
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
|
|---|---|
| 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 | 0.5879 mL | 2.9396 mL | 5.8791 mL | |
| 5 mM | 0.1176 mL | 0.5879 mL | 1.1758 mL | |
| 10 mM | 0.0588 mL | 0.2940 mL | 0.5879 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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