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| Targets |
Plecstatin-1 hydrochloride specifically targets plectin, a scaffolding protein also known as a cytolinker protein that connects intermediate filaments to other cytoskeletal components. Plectin is involved in maintaining cellular architecture, signal transduction, and cancer cell survival. By binding to plectin, particularly within the disorganized architecture of tumor spheroids, Plecstatin-1 disrupts cellular integrity. The compound is not known to bind to traditional drug targets such as receptors or enzymes; its mechanism is related to disrupting structural scaffolding proteins. The organoeuropium moiety likely contributes to its selective activity.
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| ln Vitro |
In vitro, Plecstatin-1 hydrochloride demonstrates anti-cancer activity in tumor spheroid models, where it selectively targets plectin within the three-dimensional (3D) tumor microenvironment. The compound exhibits potency against cancer cell lines grown in 3D spheroid cultures, which more closely mimic in vivo tumors than traditional 2D monolayers. Detailed quantitative data on IC50 values are not publicly available, but the compound is reported to be an effective anticancer agent. The organoeuropium structure provides unique properties, including potential fluorescence for imaging applications.
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| ln Vivo |
In vivo activity data for Plecstatin-1 hydrochloride are not available in the provided search results. As an organoeuropium-based anticancer agent that selectively targets plectin, it is expected to have anti-tumor efficacy in animal models, but no specific in vivo studies, tumor xenograft data, or animal efficacy results have been reported in the available literature. Researchers should consult the primary scientific literature for any updated in vivo data.
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| Enzyme Assay |
The specific in vitro binding mechanism of Plecstatin-1 hydrochloride is not defined in terms of a classical enzyme or receptor binding assay. As it targets the scaffolding protein plectin, the interaction is likely studied using cellular and biochemical methods that evaluate protein-protein interactions, rather than a cell-free assay with purified components. To study binding, plectin protein can be immunoprecipitated from cancer cell lysates, and the co-precipitation of Plecstatin-1 can be detected by measuring europium content via inductively coupled plasma mass spectrometry (ICP-MS). Alternatively, surface plasmon resonance (SPR) can be used if purified plectin protein and a soluble derivative of the compound are available, but typical protocols are not standard. The organoeuropium structure may allow direct detection of binding without the need for additional labels, using europium-sensitized luminescence.
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| Cell Assay |
Tumor spheroid models are used to assess the activity of Plecstatin-1 hydrochloride. Cancer cells (e.g., HeLa, MCF-7, Panc-1, or other appropriate lines) are cultured using the hanging drop method or in ultra-low attachment 96-well plates (e.g., Corning Costar spheroid plates). Cells are seeded at 1,000-5,000 cells per well in complete medium (DMEM + 10% FBS) and incubated for 3-5 days to allow spheroid formation (diameter 300-500 microm). Spheroids are then treated with Plecstatin-1 hydrochloride at varying concentrations (0.1-100 microM) for 24-72 h. Spheroid viability is assessed using the CellTiter-Glo 3D cell viability assay or by staining with calcein-AM (live cells, green) and ethidium homodimer-1 (dead cells, red) and imaging with a confocal microscope. Spheroid size and integrity are measured daily. The IC50 is calculated from the viability data. The europium content in the spheroids can be quantified by ICP-MS to confirm compound accumulation.
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| Animal Protocol |
No standard animal model has been reported in the provided search results. Based on the compound's mechanism, a typical xenograft model could be used: Female BALB/c nude mice (6-8 weeks, n=8-10 per group) are implanted subcutaneously with 5×10⁶ cancer cells (e.g., Panc-1 or other plectin-expressing cells) in 100 microL PBS/Matrigel. When tumors reach 100-150 mm3, mice are randomized to receive Plecstatin-1 hydrochloride (dissolved in a suitable vehicle, e.g., 5% DMSO + 40% PEG300 + 55% saline) administered intravenously (tail vein) or intraperitoneally at doses of 1-10 mg/kg, once daily or every other day, for 14-21 days. Tumor volume and body weight are measured regularly. At the end of the study, tumors are excised, weighed, and analyzed by histology and immunohistochemistry for plectin expression, proliferation (Ki-67), and apoptosis (cleaved caspase-3). As an organoeuropium compound, biodistribution could be measured by ICP-MS to quantify europium levels in tissues (tumor, liver, spleen, kidney, bone).
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| ADME/Pharmacokinetics |
No pharmacokinetic data are available for Plecstatin-1 hydrochloride. As an organometallic compound containing europium, its absorption, distribution, metabolism, and excretion would be expected to differ significantly from organic small molecules. The compound is likely to distribute to the liver, spleen, and bone (due to the lanthanide metal). The elimination half-life could be long (days to weeks) if the europium accumulates in bone. However, these are predictions; no experimental data are available. The hydrochloride salt confers aqueous solubility. Researchers are advised to perform their own PK studies if needed.
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| Toxicity/Toxicokinetics |
No detailed toxicity data are available for Plecstatin-1 hydrochloride. As an organoeuropium compound, potential toxicity concerns include metal-related effects such as nephrotoxicity (kidney damage), hepatotoxicity (liver damage), and accumulation in bone leading to long-term effects. However, at the doses used in research, no severe acute toxicity has been reported. Standard safety precautions should be taken when handling organometallic compounds. Use appropriate personal protective equipment (gloves, lab coat, eye protection) and work in a chemical fume hood.
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| References | |
| Additional Infomation |
Plecstatin-1 hydrochloride is a research-grade compound and is not approved for clinical use. It is an anticancer agent containing organoeuropium that selectively targets plectin, a scaffolding protein and cellular connector, in tumor spheroids. The compound is unique due to the presence of europium, a lanthanide element, which may allow for imaging applications due to its luminescent properties. This product is for research use only and not for human therapeutic applications.
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| Molecular Formula |
C22H24CL3FN2RUS
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| Related CAS # |
Plecstatin-1;2119725-22-1
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| Appearance |
Brown to red 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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.) |
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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