| Chemical Properties | Back Directory | [Boiling point ]
542.8±60.0 °C(Predicted) | [density ]
1.56±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
9.43±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
SHP289-04 is a novel glucokinase activator (gka), accelerating glucose consuming in hepatocytes, promoting glucose-stimulated insulin secretion in nit cell line. normalizing oral glucose tolerance test and down-regulated blood lipid level in kkay mice | [Uses]
SHP394 is an orally active, selective and allosteric inhibitor of SHP2, with an IC50 of 23 nM[1]. | [in vivo]
SHP394 (20-80 mg/kg; oral gavage; twice daily) dose-dependent reduces tumor volume[1].
SHP394 (80 mg/kg; oral gavage; twice daily) causes tumor 34% regression and reduces mouse host bodyweight after dosing for 14 days[1].
| Animal Model: | Six-week old female athymic NU/NU mice were inoculated subcutaneously with Detroit-562 pharyngeal carcinoma cells[1]. | | Dosage: | 20, 40, and 80 mg/kg | | Administration: | Oral gavage; twice daily | | Result: | Demonstrated a clear dose-dependent reduction in tumor volume. |
| [References]
[1] Sarver P, et al. 6-Amino-3-methylpyrimidinones as Potent, Selective, and Orally Efficacious SHP2 Inhibitors. J Med Chem. 2019 Feb 28;62(4):1793-1802. DOI:10.1021/acs.jmedchem.8b01726 |
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