In vivo pharmacokinetics studies, SHP2-IN-13 (compound 129) (IV/PO; 5mg/kg) demonstrates high clearance, a high volume of distribution (13.9 L/kg), a moderate half-life (T1/2=5.31 h). Additionally, SHP2-IN-13 shows a higher oral bioavailability (F =55.07 ± 7.93%) than SHP099 (F =46%) and is suitable for further in vivo anti-tumor evaluation[1].
SHP2-IN-13 (oral gavage; 20 mg/kg; daily) exhibits an anti-leukaemic efficacy and causes significant reduction of leukemia burden. Additionally, it near completely eradicated human CD45+ leukaemic cells in blood and spleen[1].
| Animal Model: | Murine NSG xenograft model inoculated with FLT3-ITD mutated MV-4-11-luciferase (MV-4-11-Luc) AML cells[1] |
| Dosage: | 20 mg/kg |
| Administration: | Oral gavage; 20 mg/kg; daily |
| Result: | Exhibited an anti-tumour efficacy in AML model. |