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| 10mg |
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| Targets |
The primary targets of ROS-ERS inducer 1 are reactive oxygen species (ROS) and the endoplasmic reticulum (ER). The compound engages in redox reactions within cellular environments, leading to increased levels of ROS. It successfully induces ER stress accompanied by ROS production in HCC cells. This dual mechanism ultimately triggers immunogenic cell death.
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| ln Vitro |
In vitro, ROS-ERS inducer 1 successfully induces ER stress accompanied by ROS generation in HCC cells, leading to the release of damage-associated molecular patterns (DAMPs). It displays much higher anticancer activities than Cisplatin, indicating superior cytotoxicity against liver cancer cells. The compound's mechanism involves the disruption of cellular redox balance and protein folding homeostasis.
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| ln Vivo |
In vivo activity data for ROS-ERS inducer 1 have not been detailed in the available literature. As a type II ICD inducer, it is hypothesized to have significant anti-tumor effects in animal models of hepatocellular carcinoma by triggering both ROS production and ER stress, leading to immunogenic cell death. Further in vivo validation is required.
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| Enzyme Assay |
A typical ROS detection assay in cell-free systems can be performed using a fluorescent probe such as DCFH-DA. The compound is incubated with a ROS-generating system (e.g., H2O2/Fe2+) in a buffer solution. The fluorescence (ex/em = 488/525 nm) is measured to quantify ROS generation. Alternatively, an ELISA-based assay can be used to detect ER stress markers (e.g., GRP78, CHOP) in cell lysates.
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| Cell Assay |
Hepatocellular carcinoma (HCC) cells (e.g., HepG2 or Huh7) are seeded in 96-well plates (1×10⁴ cells/well). After 24 h, cells are treated with varying concentrations (0.1-10 microM) of ROS-ERS inducer 1 for 24-48 h. Cell viability is assessed by MTT or CellTiter-Glo assay. Intracellular ROS levels are measured using the DCFH-DA probe. ER stress is evaluated by detecting GRP78 and CHOP expression via Western blot. DAMPs such as HMGB1 and ATP release are quantified by ELISA.
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| Animal Protocol |
In a standard mouse xenograft model, female BALB/c nude mice (6-8 weeks, n=8 per group) are implanted subcutaneously with 5×10⁶ HCC cells (e.g., HepG2). When tumors reach 100-150 mm3, mice are randomized and treated intraperitoneally with ROS-ERS inducer 1 (2-10 mg/kg) dissolved in a suitable vehicle (e.g., 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% saline) every 3 days for 14-21 days. Tumor volume and body weight are measured every 2-3 days. At the end of the study, tumors are excised and analyzed for ROS levels, ER stress markers, and DAMPs by Western blot and ELISA.
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| ADME/Pharmacokinetics |
ROS-ERS inducer 1 has a molecular weight of 840.35 (C24H23F12N3Pt). The powder should be stored at -20degC for up to 3 years, and at 4degC for up to 2 years. In solvent, it is stable for 6 months at -80degC. The compound is a Pt(II) complex and requires caution during handling. Detailed pharmacokinetic parameters (t½, Cmax, AUC) have not been reported.
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| Toxicity/Toxicokinetics |
Preliminary toxicity data indicate that ROS-ERS inducer 1 displays much higher anticancer activities than Cisplatin, suggesting it may have a superior therapeutic index. However, as a Pt(II) complex, standard heavy metal toxicities (nephrotoxicity, myelosuppression) must be considered. Formal toxicology studies (e.g., 28-day repeat-dose, genotoxicity) have not been published. Standard safety precautions for handling Pt(II) complexes should be followed.
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| References | |
| Additional Infomation |
ROS-ERS inducer 1 is a research-grade compound and is not approved for clinical use. It is a novel Pt(II)-NHC complex that induces immunogenic cell death via ROS generation and ER stress, making it a promising candidate for cancer immunotherapy research. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C24H23F2I2N3PT
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| Molecular Weight |
840.35
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| Appearance |
Light yellow to yellow 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)
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| Solubility (In Vitro) |
DMSO :~60 mg/mL (~71.40 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 | 1.1900 mL | 5.9499 mL | 11.8998 mL | |
| 5 mM | 0.2380 mL | 1.1900 mL | 2.3800 mL | |
| 10 mM | 0.1190 mL | 0.5950 mL | 1.1900 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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