| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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GB1107 (GB-1107) is a novel, potent, selective, orally bioavailable galectin-3 (GAL-3) inhibitor with anticancer activity. IT inhibits GAL-3 with a Kd of 37 nM. GB1107 inhibits lung adenocarcinoma growth and augments response to PD-L1 blockade. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model.
| 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].
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| 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].
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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. |
| References |
[1]. Vuong L, et al. An orally active galectin-3 antagonist inhibits lung adenocarcinoma growth and augments response to PD-L1 blockade. Cancer Res. 2019 Jan 23. pii: canres.2244.2018.
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| Molecular Formula |
C20H16CL2F3N3O4S
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|---|---|
| Molecular Weight |
522.324952125549
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| CAS # |
1978336-61-6
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| SMILES |
O[C@H]([C@@H](N1N=NC(C2=CC(F)=C(F)C(F)=C2)=C1)[C@H]([C@@H](CO)O3)O)[C@H]3SC4=CC=C(Cl)C(Cl)=C4
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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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| 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 : ~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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