Biological Activity
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.
Chemical Information
Molecular Weight |
522.32 |
Formula |
C20H16Cl2F3N3O4S |
CAS Number |
1978336-61-6
|
Purity |
>99% |
Solubility |
DMSO 45 mg/mL |
Storage |
-20°C, dry, sealed
|
References
[1] Lynda Vuong, et al. Cancer Res. An Orally Active Galectin-3 Antagonist Inhibits Lung Adenocarcinoma Growth and Augments Response to PD-L1 Blockade