| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
IC 50: 0.025 μM (Lysine demethylase 5B, KDM5B)[1].
|
|---|---|
| ln Vitro |
KDM5B-IN-4 (20 μM, 72 h) stimulates the synthesis of H3K4me1/2/3 in PC-3 cells and has a specific inhibitory effect on KDM5B [1]. In addition to targeting KDM5B in cells, KDM5B-IN-4 (0–20 μM; 72 h) causes PC-3 cells to accumulate H3K4me1/2/3 [1]. KDM5B-IN-4 (0-10 μM, 0-24 h) suppresses prostate cancer cell migration and proliferation, interrupts the PC-3 cycle in the G2/M phase, and to some extent can cause PC-3 cell apoptosis. Demise [1].
|
| ln Vivo |
KDM5B-IN-4 (50 mg/kg, ig, 50 mg/kg/d, 13 days) has a somewhat greater tumor-inhibiting activity than DOX [1]. Mice treated with KDM5B-IN-4 (50 mg/kg, ig, 50 mg/kg/d, 25 days) did not exhibit any overt toxicity or adverse effects, as reported in [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: PC-3 Tested Concentrations: 0, 2.5, 5, 10, 20 μM Incubation Duration: 72 h Experimental Results: Induced the concentrations of H3K4me1/2/3 Dramatically different from those of the control, and the results obtained were similar to those obtained using the CPI-455 positive control. Had no significant effect on P110α, P85, and pAKT at low concentration levels (0-10μM), and P110α, P85, and pAKT were Dramatically diminished when 11ad was at high concentration(20 μM). Cell Migration Assay [1] Cell Types: PC-3 Tested Concentrations: 0, 5, 10 μM Incubation Duration: 0, 6, 12, 24 h Experimental Results: Inhibited colony formation in a dosedependent manner, especially at high doses(10 μM). Cell Cycle Analysis[1] Cell Types: PC-3 Tested Concentrations: 0, 2.5, 5, 10 μM Incubation Duration: 24 h Experimental Results: Blocked the cell cycle at G2/M phase in 10 μM. Apoptosis Analysis[1] Cell Types: PC-3 Tested Concentrations: 0, 2.5, 5, 10 μM Incubation Duration: 24 h Experimental Results: Induced PC-3 cell apoptosis in a dose-dependent manner(7.58%, 26.14%, 28.20%, 4 |
| Animal Protocol |
Animal/Disease Models: PC-3 xenograft model in male Spraguee-Dawley rats[1].
Doses: 25, 50 mg/kg Route of Administration: intragastric (po) administration to mice (ig) for 25 days, administered one time/day. Experimental Results: Compared with NaCl treatment, treatment with 25 mg/kg and 50 mg/kg Dramatically diminished tumor volume. Animal/Disease Models: PC-3 xenograft model in male Spraguee-Dawley rats[1]. Doses: 2 g/kg Route of Administration: intragastric (po) administration to mice (ig) for 14 days, administered one time/day. Experimental Results: No significant loss of major organs in the high-dose and low-dose groups. |
| References |
| Molecular Formula |
C30H30N6O
|
|---|---|
| Molecular Weight |
490.60
|
| Appearance |
White to off-white solid powder
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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)
|
| 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 | 2.0383 mL | 10.1916 mL | 20.3832 mL | |
| 5 mM | 0.4077 mL | 2.0383 mL | 4.0766 mL | |
| 10 mM | 0.2038 mL | 1.0192 mL | 2.0383 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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