| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Other Sizes |
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| ln Vitro |
Skp2-Cks1 communication is disrupted by Skp2 inhibitor 1 (2.8 μM, 72 hours), with IC50 values of 4.8 μM and 7.0 μM for PC-3 and MGC-803 cells, respectively [1]. Inhibitor 1 for Skp2 (10 μM, 48 hours). causes cell arrest in the S phase, stimulates cell growth, and inhibits PC-3 and MGC-803 cell migration and proliferation [1].
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| ln Vivo |
In the NOD-SCID mouse xenograft model, Skp2 inhibitor 1 (10 mg/kg; 25 mg/kg, 50 mg/kg; intraperitoneal injection/2 days, 21 days) significantly inhibited tumor growth without obvious toxicity. Furthermore, the growth of tumors was totally inhibited by treatment with Skp2 Skp2 inhibitor 1 (50 mg/Kg/2 days) [1]. By blocking Skp2 signaling dye, Skp2 inhibitor 1 decreases the size of tumors and increases the percentage of cells in tumor tissue [1]. Xenograft model of MGC-803 cells and NOD-SCID mouse PC-3 [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: PC-3, MGC-803 Tested Concentrations: 0- 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: IC50 value for Skp2−Cks1 interaction is 2.8 μM, against PC-3 and MGC-803 The IC50 values for cells were 4.8 and 7.0 μM, respectively. Apoptosis analysis [1] Cell Types: PC-3, MGC-803 Tested Concentrations: 2.5 μM, 5 μM, 10 μM Incubation Duration: 0-48 h Experimental Results: Caused cell cycle S phase arrest in a dose-dependent manner, and Apoptosis, such as nuclear fragmentation, condensation, and cell shrinkage, is induced in a dose-dependent manner. Cell proliferation assay[1] Cell Types: PC-3, MGC-803 Tested Concentrations: 0.5 μM, 1 μM, 2 μM Incubation Duration: 10 days Experimental Results: Inhibition of colony-forming ability in a dose-dependent manner. Cell migration assay[1] Cell Types: PC-3, MGC-803 Tested Concentrations: 2.5 μM, 5 μM, 10 μM Incubation Duration: 48 h Experimental Results: Inhibition of migration in a dose-dependent manner. Cell invasion experiment [1] Cell Types: PC-3, MGC-803 Tested Concentrations: 0.5 μM, 1 μM, 2 μM Incubation time |
| Animal Protocol |
Animal/Disease Models: The xenograft models of PC-3 and MGC-803 cells in NOD-SCID (severe combined immunodeficient) mouse[1].
Doses: 10 mg/kg; 25 mg/kg, 50 mg/kg Route of Administration: intraperitoneal (ip) injection (i.p.) Experimental Results:Inhibited tumor growth without obvious toxicity, the tumor growth inhibition ratio was 55.68, 71.86, and 90.42% with 10, 25, and 50 mg/Kg/2 day, respectively. |
| References |
[1]. Zhang K, et al. Discovery of Novel 1,3-Diphenylpyrazine Derivatives as Potent S-Phase Kinase-Associated Protein 2 (Skp2) Inhibitors for the Treatment of Cancer. J Med Chem. 2023 Jun 8;66(11):7221-7242.
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| Molecular Formula |
C23H23CLN4O
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|---|---|
| Molecular Weight |
406.907923936844
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| Exact Mass |
406.16
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| Elemental Analysis |
C, 67.89; H, 5.70; Cl, 8.71; N, 13.77; O, 3.93
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| CAS # |
2760612-63-1
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| PubChem CID |
162718203
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
29
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| Complexity |
513
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MKWLNXUIWPRODH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H23ClN4O/c24-15-21(29)26-19-11-13-28(14-12-19)20-16-25-22(17-7-3-1-4-8-17)23(27-20)18-9-5-2-6-10-18/h1-10,16,19H,11-15H2,(H,26,29)
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| Chemical Name |
2-chloro-N-(1-(5,6-diphenylpyrazin-2-yl)piperidin-4-yl)acetamide
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| Synonyms |
Skp2 inhibitor 1; Skp2 inhibitor-1; Skp2-inhibitor 1; compound 14i
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~122.88 mM)
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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 | 2.4575 mL | 12.2877 mL | 24.5755 mL | |
| 5 mM | 0.4915 mL | 2.4575 mL | 4.9151 mL | |
| 10 mM | 0.2458 mL | 1.2288 mL | 2.4575 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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