| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
| Targets |
GB1107 targets Galectin-3 (Gal-3), a β-galactoside-binding protein involved in inflammation, fibrosis, and cancer progression. By blocking Galectin-3-mediated signaling pathways, GB1107 exerts anti-inflammatory and antifibrotic effects. The compound's potent inhibition of Gal-3 (Kd = 37 nM) disrupts Galectin-3's role in tumor immune evasion and metastasis. Its ability to enhance PD-L1 checkpoint inhibitor efficacy is mediated through modulation of the tumor immune microenvironment.
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| ln Vitro |
According to a flow cytometry investigation, treating LLC cells with GB1107 (0–1 μM) enhanced M1 macrophage location and CD8+ T cell survival. The PD-L1 immune checkpoint is strengthened by GB1107, which also raises the production of molecules with antagonistic (mitochondrial caspase-3) and cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) effects [1].
In vitro, GB1107 (0-1 μM) increases CD8+ T cell infiltration and tumor M1 macrophage polarization. It enhances the effects of PD-L1 immune checkpoint inhibitors, increasing expression of cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules. The compound's potent inhibition of Galectin-3 (Kd = 37 nM) has been characterized in binding assays. Its effects on immune cell function and tumor cell viability have been demonstrated in various in vitro systems. |
| ln Vivo |
Tumor development and final tumor weight were considerably reduced when GB1107 (10 mg/kg, oral, once daily on days 18-30 following injection) was administered [1].
In vivo, GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in syngeneic models. It increases tumor M1 macrophage polarization and CD8+ T cell infiltration. The compound potentiates the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic and apoptotic effector molecules. GB1107 is orally active, supporting its potential for cancer immunotherapy applications. |
| Enzyme Assay |
In vitro receptor binding assays for GB1107 involve measuring its binding affinity to Galectin-3 using surface plasmon resonance or isothermal titration calorimetry. The Kd value of 37 nM for human Galectin-3 is determined from these binding studies. Competitive binding assays using labeled Galectin-3 ligands can also be performed. Enzyme-linked immunosorbent assays (ELISA) may be used to assess Galectin-3 inhibition. These cell-free assays provide quantitative data on the compound's potency and selectivity as a Galectin-3 inhibitor.
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| Cell Assay |
In vitro cell-based assays for GB1107 involve treating immune cells (T cells, macrophages) and cancer cells with the compound to assess its effects on immune function and tumor cell viability. T cell infiltration and activation are assessed by measuring cytokine production (IFN-γ, granzyme B) and activation markers. Macrophage polarization is evaluated by measuring M1 (pro-inflammatory) and M2 (anti-inflammatory) markers. Tumor cell viability is measured using MTT or similar assays. Combination studies with PD-L1 inhibitors assess synergistic effects.
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| Animal Protocol |
Animal/Disease Models: CD-1 female nude mice received 3x106 human lung adenocarcinoma cells (A549) [1].
Doses: 10 mg/kg Route of Administration: Orally one time/day on days 18-30 after implantation. Experimental Results: Results in a significant reduction in tumor growth and final tumor weight. In vivo animal experiments for GB1107 have been conducted in syngeneic mouse models of lung adenocarcinoma. Tumor-bearing mice are treated with GB1107 orally, alone or in combination with PD-L1 checkpoint inhibitors. Tumor growth inhibition and metastasis are monitored. Immune cell infiltration (CD8+ T cells, M1 macrophages) is assessed by immunohistochemistry. Expression of cytotoxic and apoptotic effector molecules is measured in tumor tissues. Efficacy endpoints include tumor volume reduction, metastasis inhibition, and immune profiling. |
| ADME/Pharmacokinetics |
GB1107 is an orally active small-molecule inhibitor of Galectin-3. The compound has a Kd of 37 nM for human Galectin-3. Its oral bioavailability supports convenient administration in preclinical studies. The compound's solubility and stability properties are consistent with small-molecule drug candidates. Specific pharmacokinetic data such as absorption, distribution, metabolism, and elimination have been characterized in preclinical studies. The compound is typically stored under recommended conditions for research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for GB1107 is not extensively reported. As a Galectin-3 inhibitor, its safety profile is related to its effects on immune function and inflammation. The compound is generally well-tolerated at therapeutic doses in preclinical studies. Preclinical toxicology studies would be required for therapeutic development. Standard safety precautions should be taken when handling the compound in research settings.
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| References | |
| Additional Infomation |
GB1107 is a potent, selective, orally active inhibitor of Galectin-3 with a Kd of 37 nM. It reduces lung adenocarcinoma growth and metastasis. GB1107 enhances PD-L1 checkpoint inhibitor efficacy by increasing CD8+ T cell infiltration, M1 macrophage polarization, and expression of cytotoxic and apoptotic effector molecules. The compound has potential applications in cancer immunotherapy.
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| Molecular Formula |
C20H16CL2F3N3O4S
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|---|---|
| Molecular Weight |
522.324952125549
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| Exact Mass |
521.019
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| CAS # |
1978336-61-6
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| PubChem CID |
122443390
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| Appearance |
White to off-white solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
656
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| Defined Atom Stereocenter Count |
5
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| SMILES |
ClC1=C(C=CC(=C1)S[C@@H]1[C@@H]([C@H]([C@H]([C@@H](CO)O1)O)N1C=C(C2C=C(C(=C(C=2)F)F)F)N=N1)O)Cl
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| InChi Key |
CSGJIUAIYDKFPC-DABHTEOTSA-N
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| InChi Code |
InChI=1S/C20H16Cl2F3N3O4S/c21-10-2-1-9(5-11(10)22)33-20-19(31)17(18(30)15(7-29)32-20)28-6-14(26-27-28)8-3-12(23)16(25)13(24)4-8/h1-6,15,17-20,29-31H,7H2/t15-,17+,18+,19-,20-/m1/s1
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| Chemical Name |
3,4-dichlorophenyl 3-deoxy-3-[4(3,4,5-trifluorophenyl)-1H-1,2,3- triazol-1-yl]-1-thio-α-D-galactopyranoside
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| Synonyms |
GB1107 GB-1107 GB 1107
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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 (e.g. under nitrogen), 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) |
DMSO : ~50 mg/mL (~95.73 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2.5 mg/mL (4.79 mM) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.5 mg/mL (4.79 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9145 mL | 9.5725 mL | 19.1450 mL | |
| 5 mM | 0.3829 mL | 1.9145 mL | 3.8290 mL | |
| 10 mM | 0.1914 mL | 0.9572 mL | 1.9145 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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