| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Peptide E5 (0.1 μM; 40 min) exhibits specific binding affinity to CXCR4-overexpressing 4T1 breast cancer cells and HUVEC cells, but lacks this binding activity to MS-5 cells with low CXCR4 expression [1]. Peptide E5 (0-100 μM; 24 h) induces cytotoxicity and apoptosis in 4T1 cells in a concentration-dependent manner [1]. Peptide E5 (0.1-10 μM; 1 h pre-incubation) inhibits CXCL12-induced migration of 4T1 breast cancer cells and HUVEC cells, as well as 4T1 cell migration induced by MS-5 conditioned medium [1]. Peptide E5 (0.1-10 μM; 2 h pre-incubation) inhibits the adhesion of 4T1 breast cancer cells to MS-5 stromal cells in a concentration-dependent manner [1].
|
|---|---|
| ln Vivo |
Peptide E5 (40 mg/kg; subcutaneous injection; every other day; days 7-33) showed weak antitumor activity as a single drug, but it could significantly enhance the antitumor efficacy of paclitaxel and cyclophosphamide [1]. Peptide E5 (40 mg/kg; subcutaneous injection; single dose) had a long half-life (about 10 hours) in healthy female BALB/c mice and was mainly eliminated by liver metabolism [1].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: Mouse breast cancer 4T1 cells, HUVEC cells Tested Concentrations: 0, 1, 10, 25, 50 and 100 μM Incubation Duration: 24 hours Experimental Results: At concentrations <25 μM, 4T1 cell viability remained above 90%. At 50 μM, 75 μM and 100 μM, 4T1 cell viability decreased to 72%, 57% and 49%, respectively. At all test concentrations (up to 100 μM), HUVEC cell viability remained above 90%. Western Blot analysis [1] Cell Types: Mouse breast cancer 4T1 cells Tested Concentrations: 0, 1, 10, 25, 50 and 100 μM Incubation Duration: 24 hours Experimental Results: Increased the level of cleaved caspase-3. |
| Animal Protocol |
Animal/Disease Models:BALB/c (female, 5-6 weeks old, orally inoculated with 1×10⁶ 4T1 mouse breast cancer cells)[1]
Doses: 40 mg/kg Route of Administration: Subcutaneous injection; every other day; days 7-33 Experimental Results: When administered alone, no significant inhibitory effect on tumor weight was observed compared with the control group. When combined with paclitaxel, tumor weight was significantly reduced compared with the control group and the paclitaxel monotherapy group. Compared with the cyclophosphamide monotherapy group, tumor weight was significantly reduced and survival was prolonged. When administered alone or in combination with paclitaxel or cyclophosphamide, the expression level of CD31 in tumor tissue was significantly reduced. When combined with paclitaxel or cyclophosphamide, the expression of CXCR4 in tumor tissue was downregulated. When used alone or in combination with cyclophosphamide, it can significantly inhibit the phosphorylation of Akt and Erk in tumor tissue. |
| References |
| Molecular Formula |
C113H181N39O31S
|
|---|---|
| Molecular Weight |
2613.95
|
| CAS # |
1643580-44-2
|
| Sequence |
Gly-Gly-Arg-Ser-Phe-Phe-Leu-Leu-Arg-Arg-Ile-Gln-Gly-Cys-Arg-Phe-Arg-Asn-Thr-Val-Asp-AspGGRSFFLLRRIQGCRFRNTVDD
|
| SequenceShortening |
GGRSFFLLRRIQGCRFRNTVDD
|
| Appearance |
Typically exists as solids 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) |
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 | 0.3826 mL | 1.9128 mL | 3.8256 mL | |
| 5 mM | 0.0765 mL | 0.3826 mL | 0.7651 mL | |
| 10 mM | 0.0383 mL | 0.1913 mL | 0.3826 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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