| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PeS-9 (48 hours) showed cytotoxicity against cancer cells with IC50 values of 0.49 μM (DU145) and 0.58 μM (LNCaP), respectively, while exhibiting lower cytotoxicity against non-cancer cells with IC50 values of 3.41 μM (PNT2), 3.53 μM (MRC-9), 11.7 μM (HUVEC), and 7.51 μM (HEK)[1]. PeS-9 (0-2.5 μM, 4-48 hours) downregulated the androgen receptor (AR) signaling pathway in 22Rv1 cells, generating reactive oxygen species (ROS) and damaging DNA[1]. PeS-9 (48 hours) had a synergistic effect with the anti-androgen enzalutamide and the PARP inhibitor olaparib in 22Rv1 cells, CI < 0.75[1]. PeS-9 (0-1 μM, 1 h) activates the MAPK signaling pathway by increasing the levels of stress kinases p-p38, p-JNK, and p-ERK in 22Rv1 cells, and this activation can be antagonized by the tested MAPK inhibitors [1]. PeS-9 (0-2.5 μM, 1-48 h) induces apoptosis in 22Rv1 cells by targeting mitochondria and inducing cytotoxic ROS [1]. PeS-9 (0-2.5 μM, 1-48 h) leads to increased cytoplasmic Ca2+ levels, endoplasmic reticulum (ER) dilation, altered mitochondrial membrane permeability, and DNA damage, manifested as an increased proportion of cells in the sub-G1 phase [1]. PeS-9 (0.5-4 μM, 24 h) inhibits glucose uptake in 22Rv1 cells, an effect that can be inhibited by the GLUT-1 inhibitor Phloretin [1]. PeS-9 (0.1–10 μM, every 5 days for 20 days) reduced tumor-like survival in a dose-dependent manner [1].
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|---|---|
| ln Vivo |
PeS-9 (27.9 mg/kg, intraperitoneal injection, once daily for 15 days) exhibited antitumor and antimetastatic activity in immunodeficient NOD/SCID gamma (NSG) mice with subcutaneous transplantation of human prostate cancer 22Rv1 cells, with relatively few side effects [1].
|
| Cell Assay |
Western Blot analysis [1]
Cell Types: 22Rv1 cells Tested Concentrations: 1, 2 μM Incubation Duration: 48 hours Experimental Results: AR-FL, AR-V7, PSA, and IGF-1 proteins were downregulated in a dose-dependent manner. Real-time quantitative PCR[1] Cell Types: 22Rv1 cells Tested Concentrations: 0, 0.5, 1, 2 μM Incubation Duration: 48 hours Experimental Experimental Results: The transcription of TMPRSS2, FKBP5 and PSA genes was inhibited in a dose-dependent manner. Immunofluorescence [1] Cell Types: 22Rv1 cells Tested Concentrations: 1.25, 2.5 μM Incubation Duration: 4, 24 hours, 48 hours Experimental Results: Induced DNA double-strand breaks (DSBs), as shown by the formation of γH2AX/53BP1 focal points. Primary DNA damage was triggered within 4 hours after treatment, peak damage was reached at 24 hours, and signs of DNA repair activation were observed at 48 hours.
|
| Animal Protocol |
Animal/Disease Models:NOD/SCID gamma (NSG) mice aged 8–12 weeks with subcutaneous transplantation of human prostate cancer 22Rv1 cells[1].
Doses: 27.9 mg/kg Route of Administration: Intraperitoneal injection daily for 15 consecutive days Experimental Results: Tumor volume was reduced by 40.0% (1069.5 mm³ vs. 646.6 mm³) compared to the control group. Lung micrometastases were reduced by 4.4-fold. There were no significant differences in body weight, heart, lung, liver, and kidney weight. Splenomegaly was observed, indicating an immunostimulatory effect of the treatment. There were no significant differences in white blood cell, red blood cell, platelet, hemoglobin, and hematocrit levels. No signs of tissue damage, inflammation, or granulomas were observed. |
| References |
| Molecular Formula |
C26H28O13S
|
|---|---|
| Molecular Weight |
580.56
|
| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
COC1=C(CSC[C@H]2O[C@H]([C@@H]([C@H]([C@@H]2OC(C)=O)OC(C)=O)OC(C)=O)OC(C)=O)C(C3=C(C=CC=C3O)C1=O)=O
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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) |
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 | 1.7225 mL | 8.6124 mL | 17.2247 mL | |
| 5 mM | 0.3445 mL | 1.7225 mL | 3.4449 mL | |
| 10 mM | 0.1722 mL | 0.8612 mL | 1.7225 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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