| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
SeSA-HCPT (48 hours) exhibited excellent selective cytotoxicity against AR-positive (LNCaP) and AR-negative (PC3, DU145) human prostate cancer cells, with IC50 values of 0.182, 0.198 and 0.175 μM, respectively, and extremely low cytotoxicity against normal human keratinocytes HaCaT (IC50 = 5.17 μM) [1]. SeSA-HCPT (200 nM; 24-48 hours) significantly induced apoptosis in PC3, DU145 and LNCaP human prostate cancer cells [1]. SeSA-HCPT (0.175-5.17 μM; 24 hours) induced S-phase cell cycle arrest in PC3, DU145 and LNCaP human prostate cancer cells, had no effect on normal human keratinocytes HaCaT, and upregulated the expression of cyclin E in PC3 and DU145 cells [1]. SeSA-HCPT (3-10 μM) inhibits topoisomerase I (TopoI)-mediated DNA relaxation and has a higher affinity for the TopoI-DNA complex than HCPT, thereby enhancing its ability to block the catalytic function of TopoI [1]. SeSA-HCPT (1.25-5 nM) inhibits histone deacetylase (HDAC) activity in PC3 and DU145 human prostate cancer cells [1]. SeSA-HCPT (1.25-5 nM) can induce dose-dependent DNA damage in PC3 and DU145 human prostate cancer cells, manifested as an increase in γ-H2AX levels [1]. SeSA-HCPT (5 nM; 24-48 h) significantly inhibits the proliferation and migration of PC3 and DU145 human prostate cancer cells [1]. SeSA-HCPT (0-50 nM; 24 hours) impaired homologous recombination-mediated DNA repair in PC3 and DU145 human prostate cancer cells by downregulating KIF4A and reducing Rad51 recruitment to DNA damage sites, while inducing DNA damage responses and causing a dose-dependent decrease in KIF4A levels from 0 nM to 50 nM [1].
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|---|---|
| ln Vivo |
SeSA-HCPT (20 mg/kg; ig; single dose) can effectively inhibit the growth of castration-resistant prostate cancer xenografts, reduce tumor cell proliferation, induce DNA damage, and has minimal systemic toxicity [1].
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: PC3, DU145, LNCaP cells Tested Concentrations: 200 nM (Annexin V/PI staining); 200 nM (Western blot) Incubation Duration: 48 hours (Annexin V/PI staining); 24 hours (Western blot) Experimental Results: A significantly increased level of apoptosis was induced. The levels of cleaved caspase-3 and p21 were increased in all three cell lines. Cell cycle analysis [1] Cell Types: PC3, DU145, LNCaP, HaCaT cells Tested Concentrations: 0.175, 0.182, 0.198, 5.17 μM Incubation Duration: 24 hours Experimental Results: Significantly induced S-phase arrest in PC3, DU145, and LNCaP cells. Upregulated the expression of cyclin E in PC3 and DU145 cells, while the levels of cyclin A2 or cyclin B did not change significantly. Did not alter the cell cycle distribution of HaCaT cells. Western Blot Analysis [1] Cell Types: PC3, DU145 cells Tested Concentrations: 1, 5, 10, 30, 50 nM Incubation Duration: 24 hours Experimental Results: γ-H2AX and phosphorylated ATM (pS1981-ATM) levels increased at 5 nM. KIF4A levels decreased from 1 to 50 nM. |
| Animal Protocol |
Animal/Disease Models:BALB/c nude mice (male, 5 weeks old, PC3 cell subcutaneous xenograft) [1]
Doses: 20 mg/kg Route of Administration: Immunoglobulin; single dose Experimental Results: Significantly reduced tumor weight and growth. Significantly reduced Ki67-positive cells. Significantly increased γ-H2AX-positive cells. No significant difference in body weight compared to the control group. No significant changes in liver (ALT, AST, ALP) or kidney (BUN, creatinine) indicators. |
| References |
| Molecular Formula |
C76H76N6O18SE2
|
|---|---|
| Molecular Weight |
1519.37
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NC1=CC(COC(CCC(OC2=C(C=C(CN3C4=CC5=C(COC(C5(CC)O)=O)C3=O)C4=N6)C6=CC=C2)=O)=O)=CC=C1)CCCCCC[Se][Se]CCCCCCC(NC7=CC(COC(CCC(OC8=C9C=C%10CN%11C(C%12=C(C=C%11C%10=NC9=CC=C8)C(O)(C(OC%12)=O)CC)=O)=O)=O)=CC=C7)=O
|
| 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
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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 | 0.6582 mL | 3.2908 mL | 6.5817 mL | |
| 5 mM | 0.1316 mL | 0.6582 mL | 1.3163 mL | |
| 10 mM | 0.0658 mL | 0.3291 mL | 0.6582 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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