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| | GB 1107) Basic information |
| Product Name: | GB 1107) | | Synonyms: | GB 1107);GB1107
(GB-1107;(2R,3R,4S,5R,6R)-2-(3,4-dichlorophenyl)sulfanyl-6-(hydroxymethyl)-4-[4-(3,4,5-trifluorophenyl)triazol-1-yl]oxane-3,5-diol;α-D-Galactopyranoside, 3,4-dichlorophenyl 3-deoxy-1-thio-3-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-;GB1107, 10 mM in DMSO;3,4-Dichlorophenyl 3-deoxy-1-thio-3-[4-(3,4,5-trifluorophenyl)-1H-1,2,3-triazol-1-yl]-α-D-galactopyranoside | | CAS: | 1978336-61-6 | | MF: | C20H16Cl2F3N3O4S | | MW: | 522.32 | | EINECS: | | | Product Categories: | | | Mol File: | 1978336-61-6.mol |  |
| | GB 1107) Chemical Properties |
| Boiling point | 740.1±70.0 °C(Predicted) | | density | 1.73±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C,protect from light | | solubility | DMSO:50.0(Max Conc. mg/mL);95.73(Max Conc. mM) | | form | Solid | | pka | 12.48±0.70(Predicted) | | color | White to off-white | | InChIKey | CSGJIUAIYDKFPC-XOZWYLPJNA-N | | SMILES | O[C@H]1[C@H](O[C@H](CO)[C@H](O)[C@@H]1N1N=NC(C2C=C(F)C(F)=C(F)C=2)=C1)SC1C=CC(Cl)=C(Cl)C=1 |&1:1,2,4,7,9,r| |
| | GB 1107) Usage And Synthesis |
| Description | GB1107 is a potent, selective, orally active galectin-3 inhibitor with Kd of 37 nM. GB1107 Inhibits Lung Adenocarcinoma Growth and Augments Response to PD-L1 Blockade. | | Uses | GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. GB1107 reduces human and mouse lung adenocarcinoma growth and blocks metastasis in the syngeneic model[1]. | | in vivo | Oral administration of a novel small molecule galectin-3 inhibitor GB1107 reduced human and mouse lung adenocarcinoma growth and blocked metastasis in the syngeneic model. Treatment with GB1107 increased tumor M1 macrophage polarization and CD8+ T-cell infiltration. Moreover, GB1107 potentiated the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic (IFNγ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules._x000D_
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Reference: Cancer Res. 2019 Apr 1;79(7):1480-1492. https://pubmed.ncbi.nlm.nih.gov/30674531/ | | target | GB1107 is a potent, selective, orally active inhibitor of Galectin-3 (Gal-3) with a Kd of 37 nM for human Galectin-3. | | IC 50 | Galectin-3 | | 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. DOI:10.1158/0008-5472.CAN-18-2244 |
| | GB 1107) Preparation Products And Raw materials |
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