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| 5mg |
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| Targets |
G3-C12 targets galectin-3 (Gal-3), a member of the galectin family of carbohydrate-binding proteins. The peptide binds to galectin-3 with high affinity, with a Kd of 88 nM. It shows no affinity for other members of the galectin family or unrelated lectins, demonstrating high selectivity. Galectin-3 is involved in various biological processes including cell adhesion, proliferation, apoptosis, and inflammation, and is overexpressed in various cancers. Through its binding to galectin-3, G3-C12 can modulate galectin-3-mediated signaling pathways and functions.
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| ln Vitro |
G3-C12 is a peptide that binds to galectin 3 with a high affinity (Kd) of 88 nM; it has no affinity for other lectins or members of the galectin family. In comparison to copolymers containing galactose, copolymer N-(2-hydroxypropyl)methacrylamide (HPMA) with G3-C12 exhibits superior galectin-3 targeting, as it can target colorectal cancer (CRC) tumor cells overexpressing galectin 3 in an efficient and selective manner [1].
In vitro studies have characterized G3-C12 as a galectin-3 binding peptide with high affinity (Kd of 88 nM). The peptide exhibits anticancer activity. It shows no affinity for other galectin family members or unrelated lectins, confirming its selectivity for galectin-3. HPMA copolymers bearing G3-C12 demonstrate superior galectin-3 targeting compared to galactose-containing copolymers, enabling efficient and selective targeting of galectin-3-overexpressing colorectal cancer cells. The peptide's high affinity and selectivity make it a valuable tool for studying galectin-3 biology. |
| ln Vivo |
In vivo studies of G3-C12 are primarily focused on its use as a targeting moiety for drug delivery. HPMA copolymers bearing G3-C12 have been shown to efficiently and selectively target galectin-3-overexpressing colorectal cancer tumors. The peptide's high affinity for galectin-3 (Kd of 88 nM) enables selective accumulation at tumor sites expressing galectin-3. The compound's anticancer activity has been demonstrated in preclinical models. Its selective targeting of galectin-3-overexpressing cells supports its potential use in cancer diagnosis and therapy.
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| Enzyme Assay |
The in vitro binding assay for G3-C12 involves surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) to measure the binding affinity between the peptide and recombinant galectin-3 protein. The peptide is immobilized on a sensor chip or injected over immobilized galectin-3, and binding kinetics are measured. The Kd of 88 nM is determined from the binding data. Competition assays can be performed using known galectin-3 ligands to confirm specificity. Selectivity is assessed by testing binding to other galectin family members and unrelated lectins. Data analysis using appropriate binding models yields affinity constants.
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| Cell Assay |
In vitro cellular assays for G3-C12 are conducted using cancer cell lines that overexpress galectin-3, such as colorectal cancer cells. Cells are treated with G3-C12 or G3-C12-conjugated polymers, and binding and uptake are assessed using fluorescently labeled peptides. Cell proliferation and viability are measured using standard assays such as MTT. The peptide's anticancer activity is evaluated by assessing apoptosis, cell cycle arrest, and inhibition of cell migration. Specificity is confirmed using galectin-3 knockdown cells or by competition with known galectin-3 ligands. Data are collected from multiple replicates.
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| Animal Protocol |
In vivo animal studies for G3-C12 are performed in mouse xenograft models of colorectal cancer or other galectin-3-overexpressing tumors. Tumor-bearing mice are administered G3-C12 or G3-C12-conjugated therapeutic agents via intravenous injection. Tumor targeting is assessed using fluorescently labeled or radiolabeled G3-C12, and biodistribution is measured. Antitumor efficacy is evaluated by measuring tumor growth inhibition, survival, and histopathological analysis. The selective targeting of galectin-3-overexpressing tumors is confirmed by comparing accumulation in galectin-3-positive versus galectin-3-negative tumors.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for G3-C12 are limited, as it is a peptide research tool. The peptide has a molecular weight of 1758.98 g/mol. As a peptide, G3-C12 would be susceptible to proteolytic degradation and rapid clearance. Its pharmacokinetic properties would be influenced by its size, charge, and stability. When conjugated to HPMA copolymers, the pharmacokinetics are altered, with prolonged circulation and enhanced tumor accumulation. Specific PK parameters are not extensively reported. The compound is for research use only.
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| Toxicity/Toxicokinetics |
Toxicology data for G3-C12 are not extensively reported. As a peptide that binds to galectin-3, the compound's safety profile would depend on the role of galectin-3 in normal physiology. Galectin-3 is involved in various biological processes, so potential off-target effects could occur. However, the peptide's high selectivity for galectin-3 (no affinity for other galectin family members) suggests a favorable specificity profile. Specific toxicity data, including LD50 values and organ toxicity profiles, are not available. Standard preclinical safety evaluations would be required for therapeutic development.
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| References | |
| Additional Infomation |
G3-C12 is a galectin-3 binding peptide with high affinity (Kd of 88 nM) and anticancer activity. It shows no affinity for other galectin family members or unrelated lectins, demonstrating high selectivity. HPMA copolymers bearing G3-C12 efficiently and selectively target galectin-3-overexpressing colorectal cancer cells. The peptide has a molecular weight of 1758.98 g/mol. G3-C12 is a research tool for studying galectin-3 biology, cancer, and inflammation.
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| Molecular Formula |
C74H115N23O23S2
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| Molecular Weight |
1758.98
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| Exact Mass |
1757.797
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| CAS # |
848301-94-0
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| Related CAS # |
G3-C12 TFA
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| PubChem CID |
137704483
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| Appearance |
White to off-white solid powder
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| LogP |
-11.8
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| Hydrogen Bond Donor Count |
25
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| Hydrogen Bond Acceptor Count |
29
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| Rotatable Bond Count |
49
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| Heavy Atom Count |
122
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| Complexity |
3710
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[ANTPCGPYTHDCPVKR]
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| InChi Key |
RXFIUXGGWIBQLE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C74H115N23O23S2/c1-35(2)56(69(115)84-42(12-6-7-21-75)61(107)85-43(73(119)120)13-8-22-81-74(78)79)92-68(114)52-16-10-24-96(52)71(117)49(33-122)91-63(109)47(29-55(103)104)87-62(108)45(27-40-30-80-34-83-40)89-70(116)57(37(4)98)93-64(110)44(26-39-17-19-41(100)20-18-39)88-66(112)50-14-9-23-95(50)54(102)31-82-60(106)48(32-121)90-67(113)51-15-11-25-97(51)72(118)58(38(5)99)94-65(111)46(28-53(77)101)86-59(105)36(3)76/h17-20,30,34-38,42-52,56-58,98-100,121-122H,6-16,21-29,31-33,75-76H2,1-5H3,(H2,77,101)(H,80,83)(H,82,106)(H,84,115)(H,85,107)(H,86,105)(H,87,108)(H,88,112)(H,89,116)(H,90,113)(H,91,109)(H,92,114)(H,93,110)(H,94,111)(H,103,104)(H,119,120)(H4,78,79,81)
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| Chemical Name |
2-[[6-amino-2-[[2-[[1-[2-[[2-[[2-[[2-[[2-[[1-[2-[[2-[[1-[2-[[4-amino-2-(2-aminopropanoylamino)-4-oxobutanoyl]amino]-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]amino]-3-sulfanylpropanoyl]amino]acetyl]pyrrolidine-2-carbonyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3-carboxypropanoyl]amino]-3-sulfanylpropanoyl]pyrrolidine-2-carbonyl]amino]-3-methylbutanoyl]amino]hexanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
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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 | 0.5685 mL | 2.8426 mL | 5.6851 mL | |
| 5 mM | 0.1137 mL | 0.5685 mL | 1.1370 mL | |
| 10 mM | 0.0569 mL | 0.2843 mL | 0.5685 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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