| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SKLB-03220 (0.5-10 μM, 3-14 days) inhibited the proliferation and colony formation of PA-1 and A2780 cells[1]. SKLB-03220 (5-40 μM, 48 hours) induced apoptosis in PA-1 cells[1]. SKLB-03220 (0-5 μM, 0-4 days) inhibited the expression of H3K27me3 in PA-1 cells[1]. SKLB-03220 (10 μM, 3 days + washout 0-4 days) achieved sustained targeted inhibition and durable antitumor effects in PA-1 cells[1].
|
|---|---|
| ln Vivo |
SKLB-03220 (75-150 mg/kg, lateral wall, twice daily for 21 days) significantly inhibited tumor growth and showed good tolerability in PA-1 cell xenograft models [1].
|
| Cell Assay |
Apoptosis Analysis[1]
Cell Types: PA-1 cells Tested Concentrations: 5, 10, 20 and 40 μM Incubation Duration: 48 h Experimental Results: Induced ovarian cancer cell apoptosis in a dose-dependent manner. Western Blot Analysis[1] Cell Types: PA-1 cells Tested Concentrations: 0, 0.3, 0.6, 1.2, 2.5 and 5 μM Incubation Duration: 0, 1, 2, 3, 4 d Experimental Results: Effectively and persistently reduced the level of H3K27me3 within the cells, without affecting the total protein quantity of EZH2. |
| Animal Protocol |
Animal/Disease Models: PA-1 cells xenograft model established in BALB/C nude mice (6 weeks)[1]
Doses: 75 and 150 mg/kg Route of Administration: Oral administration (p.o.), twice daily for 21 days Experimental Results: Significantly inhibits tumor growth in a dose-dependent manner. Reduced the Ki-67 and H3K27me3 signals and increased cleaved Caspase-3 in tumor tissues. No significant abnormalities were observed in terms of body weight, blood routine, blood biochemical indicators, and pathological sections of major organs. |
| References |
| Molecular Formula |
C33H40N4O4
|
|---|---|
| Molecular Weight |
556.70
|
| CAS # |
2852050-29-2
|
| 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 | 1.7963 mL | 8.9815 mL | 17.9630 mL | |
| 5 mM | 0.3593 mL | 1.7963 mL | 3.5926 mL | |
| 10 mM | 0.1796 mL | 0.8981 mL | 1.7963 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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