| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| ln Vitro |
CK2-TN03 (0.2-25.0 μM; 48 hours) can induce cell death in medulloblastoma DAOY cell line and various neuroblastoma cell lines in a dose-dependent manner, with EC50 values ranging from 0.31 to 1.95 μM; it has no activity against glioblastoma U87 cells (EC50 > 25 μM) [1]. CK2-TN03 (0.35-1.0 μM; 48 hours) can activate caspase 3/7 in CHP-212 neuroblastoma cells in a time-dependent manner and mainly induce caspase-dependent apoptosis [1]. CK2-TN03 (0.5-1.0 μM; 24-48 hours) can induce G2/M phase cell cycle arrest in CHP-212 neuroblastoma cells and ultimately lead to cell death [1]. CK2-TN03 (0.5 μM; 24 hours) can arrest CHP-212 neuroblastoma cells in the mitotic phase, block cell division, and induce mitotic catastrophe and cell death [1]. CK2-TN03 (0.5 μM; 48 hours) can downregulate the activity and expression of survivin in CHP-212 neuroblastoma cells by directly inhibiting CK2-mediated survivin phosphorylation and indirectly altering the AKT1/MDM2/p53 and BRD4/MYCN pathways, without altering CK2 expression [1]. CK2-TN03 (0.5 μM; 48 hours) does not affect the viability of differentiated quiescent SH-SY5Y neuroblastoma cells, which have low survivin expression levels [1]. CK2-TN03 (1-10 μM; 72 hours) can induce cell death in 160 different cancer cell lines, showing significant tumor type selectivity, especially the highest activity against melanoma, lymphoma, lung cancer, neuroblastoma, ovarian cancer, myeloma, soft tissue cancer and osteosarcoma cell lines [1]. CK2-TN03 (10 μM; 1 hour) has excellent permeability in MDCKII-MDR1 cells, with negligible efflux and no P-gp substrate activity [1].
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| ln Vivo |
CK2-TN03 (40 mg/kg; intraperitoneal injection; once daily; 28 days) significantly reduced the growth of neuroblastoma xenograft tumors and improved the survival rate of mice, with some mice achieving long-term tumor control or remission [1].
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| Cell Assay |
Apoptosis analysis [1]
Cell Types: Neuroblastoma CHP-212 Tested Concentrations: 0.35, 0.5 and 1.0 μM Incubation Duration: 48 hours (monitored every 2 hours) Experimental Results: Caspase 3/7 activation increased over time, with a significant increase observed from 18 hours compared to the vector control group. Co-treatment with the pan-caspase inhibitor Q-VD-OPh did not affect some cell death, while this inhibitor reduced most of the CK2-TN03-induced cell death. Cell cycle analysis [1] Cell Types: Neuroblastoma CHP-212 Tested Concentrations: 0.5 and 1.0 μM Incubation Duration: 24 hours, 48 hours Experimental Results: After 24 and 48 hours of treatment, the proportions of G2/M phase cells and sub-G1 phase (dead cells) cells increased significantly compared with the control group at both concentrations and time points. After 24 hours of treatment with 0.5 μM and 1.0 μM concentrations, the proportion of G2/M phase cells increased. After 48 hours of treatment with both concentrations, the proportions of G2/M phase cells and sub-G1 phase cells further increased. Cell viability assay [1] Cell Types: Differentiated neuroblastoma SH-SY5Y Tested Concentrations: 0.5 μM Incubation Duration: 48 hours Experimental Results: The viability of differentiated SH-SY5Y cells was not reduced, and the viability protein level of the cells was approximately 20% of that of undifferentiated cells. |
| Animal Protocol |
Animal/Disease Models:(Ncr)-Foxn1 nude mice (7-8 weeks old) [1]
Doses: 40 mg/kg Route of Administration: Intraperitoneal injection; once daily for 28 days Experimental Results: Tumor growth rate decreased, and the tumor volume relative to baseline (VTx/VT0) reached approximately 6 on day 28, while it was approximately 9 in the vector control group. Mouse survival rate improved: 5 mice in the treatment group survived to day 49, while only 1 mouse in the vector control group survived; 2 mice in the treatment group survived to more than day 85, of which 1 mouse had complete tumor regression on day 14, and the other mouse had only a small amount of non-growing tumor remaining after treatment. p53 level increased in tumor tissue, while survivin level and survivin phosphorylation level decreased. |
| References |
| Molecular Formula |
C17H14N2O3S
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|---|---|
| Molecular Weight |
326.37
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| CAS # |
313226-24-3
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| Sequence |
Asp-Lys-Phe-Val-Gly-{Leu-methyl}-{Nle}-NH2DKFVG-{Leu-methyl}-{Nle}-NH2
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| SequenceShortening |
DKFVG-{Leu-methyl}-{Nle}-NH2
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| Appearance |
Light yellow to yellow solid
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| SMILES |
COC(C=C1)=C(O)C=C1/C=C(C(N/2)=O)/SC2=N\C3=CC=CC=C3
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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)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~255.32 mM; with sonication)
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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 | 3.0640 mL | 15.3200 mL | 30.6401 mL | |
| 5 mM | 0.6128 mL | 3.0640 mL | 6.1280 mL | |
| 10 mM | 0.3064 mL | 1.5320 mL | 3.0640 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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