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| 5mg |
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| Targets |
Target: MUC1-C[1]
The primary target of L-GO-203 is MUC1-C (mucin 1 C-terminal subunit), a transmembrane oncoprotein that drives tumor survival, stemness, and drug resistance by constitutively activating inflammatory signaling pathways including PI3K-AKT and NF-kappaB. |
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| ln Vitro |
L-GO-203 TFA induces the production of reactive oxygen species (ROS) and loss of mitochondrial transmembrane potential in cancer cells. At 5 uM for three days, it inhibits MUC1-positive colorectal cancer cell proliferation by decreasing intracellular glutathione levels and enhancing ROS production. It downregulates TIGAR expression.
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| ln Vivo |
In vivo animal studies demonstrate that L-GO-203 TFA significantly inhibits tumor growth and results in complete tumor regression in colon cancer xenograft models in nude mice. Administration routes include intraperitoneal or intravenous injection at doses of 3, 6, or 18 mg/kg once daily for 5-28 days.
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| Enzyme Assay |
Non-cell binding assays for MUC1-C inhibitors typically utilize recombinant MUC1-C cytoplasmic domain protein immobilized on a sensor chip for surface plasmon resonance (SPR) analysis. L-GO-203 TFA is flowed over the chip at concentrations ranging from 10 nM to 10 uM in running buffer. Binding affinity parameters are calculated by fitting the sensorgrams to a 1:1 Langmuir binding model. Alternatively, enzyme-linked immunosorbent assays (ELISA) can be performed where biotinylated MUC1-C peptide is immobilized on streptavidin-coated plates and incubated with varying concentrations of L-GO-203 to determine IC50 values for blocking the MUC1-C homodimerization interaction.
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| Cell Assay |
Cellular assays are performed using MUC1-positive cancer cell lines such as HCT116, HT-29, or MCF-7 cells. Cells are seeded in 96-well plates and treated with L-GO-203 TFA at concentrations ranging from 0.1 to 10 uM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. To evaluate ROS production, cells are incubated with 20 uM DCFH-DA for 30 minutes after compound treatment, followed by fluorescence measurement. For apoptosis detection, annexin V-FITC/PI double staining is performed followed by flow cytometry analysis. Mitochondrial membrane potential (deltaΨm) is assessed using JC-1 staining and fluorescence microscopy or flow cytometry.
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| Animal Protocol |
In vivo animal models typically employ subcutaneous xenograft models in 6-8 week old female nude mice. Approximately 5×10⁶ MUC1-positive tumor cells (e.g., HCT116 or HT-29) are implanted subcutaneously. When tumors reach approximately 100-150 mm3, mice are randomized into treatment groups (n=6-10 per group). L-GO-203 TFA is administered intraperitoneally at doses of 3, 6, or 18 mg/kg once daily for up to 28 days. Tumor volumes are measured every 2-3 days using calipers (volume = length × width2 × 0.5). Body weight is monitored for toxicity assessment. At study termination, tumors are excised, weighed, and processed for immunohistochemistry (IHC) analysis of markers including Ki-67, cleaved caspase-3, and MUC1-C expression.
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| ADME/Pharmacokinetics |
Pharmacokinetic characterization of the parent GO-203 peptide indicates that the compound is rapidly cleared from systemic circulation due to its peptide nature. The compound exhibits dose-proportional exposure following intraperitoneal administration. Peak plasma concentrations occur within 0.5-1 hour after injection. The elimination half-life in rodents is short (30-60 minutes) due to proteolytic degradation. Biodistribution studies show accumulation primarily in tumor tissues. GO-203 is known to be a cell-penetrating peptide that effectively enters cells via its poly-arginine transduction domain.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies with GO-203 demonstrate that the peptide does not lyse human red blood cells at bactericidal concentrations. In animal studies, body weight monitoring indicates that the compound is generally well-tolerated at doses up to 18 mg/kg in mice, with no significant weight loss or overt signs of toxicity observed at therapeutic doses. Higher doses may cause mild gastrointestinal disturbances. As with other peptide-based therapeutics, potential immunogenicity remains a consideration for chronic administration.
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| References | |
| Additional Infomation |
L-GO-203 TFA functions as an anticancer peptide that blocks MUC1-C homodimerization and its translocation to the nucleus. The mechanism involves binding to the CQC motif in the MUC1-C cytoplasmic domain, thereby preventing MUC1-C from forming homodimers and interacting with transcription factors. This results in downregulation of MUC1-C target genes involved in proliferation, stemness, and drug resistance. L-GO-203 has shown promise in reversing chemoresistance when combined with cisplatin. The compound is exclusively for research use and has not received regulatory approval for clinical use.
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| Molecular Formula |
C??H???F?N??O??S?
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| Molecular Weight |
2426.77
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| Related CAS # |
GO-203 TFA;1222186-26-6
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| Appearance |
White to off-white 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4121 mL | 2.0604 mL | 4.1207 mL | |
| 5 mM | 0.0824 mL | 0.4121 mL | 0.8241 mL | |
| 10 mM | 0.0412 mL | 0.2060 mL | 0.4121 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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