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. GB1107 potentiates the effects of a PD-L1 immune checkpoint inhibitor to increase expression of cytotoxic (IFN-γ, granzyme B, perforin-1, Fas ligand) and apoptotic (cleaved caspase-3) effector molecules.
| Molecular Weight | 522.32 |
| Formula | C20H16Cl2F3N3O4S |
| CAS Number | 1978336-61-6 |
| Solubility (25°C) | DMSO 45 mg/mL |
| Storage | -20°C, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Galectin Products |
|---|
| Belapectin
Belapectin, a galectin 3 inhibitor with a Ki value of 2.8 μM, reduces hepatic fibrosis and portal hypertension in rats, and can be used in studies related to non-alcoholic steatohepatitis (NASH). |
| Selvigaltin
Selvigaltin (GB1211) is an orally available galectin-3 (Gal-3) inhibitor. |
| G3-C12
G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, and shows anticancer activity. |
| OTX008
OTX008 is a selective inhibitor of galectin-1. |
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