Molecular Formula | C21H24F3N5O5S
|
Molar Mass | 515.51 |
Density | 1.483±0.06 g/cm3(Predicted) |
Boling Point | 723.1±70.0 °C(Predicted) |
Solubility | DMSO: ≥ 36 mg/mL |
pKa | 10.92±0.50(Predicted) |
Storage Condition | -20℃ |
Use | AZD3965 is a selective MCT1 inhibitor with a Ki value of 1.6 nM, which is 6 times higher than the selectivity of MCT2. |
In vitro study | AZD3965 potently inhibits lactate transport and cell growth in lymphoma cell lines preferentially expressing mct1. AZD3965 inhibits MCT1 activity in cells and shows higher sensitivity in hypoxia. In H526,HGC27 cells and DMS114 cells, AZD3965 increased intracellular lactate and significantly decreased lactate uptake. |
In vivo study | AZD3965(100 mg/kg,p.o.) reduced tumor growth and increased intratumoral lactate in non-obese diabetic SCID-γ mice bearing COR-L103 xenografts. In mice bearing H526 tumors, AZD3965(100 mg/kg, p.o.) caused increased lactate concentration, decreased growth, and increased radiosensitivity. |