Biological Activity
TNO155 is a potent selective and orally active allosteric inhibitor of wild-type SHP2 (IC50=0.011 µM). TNO155 has the potential for the study of RTK-dependent malignancies, especially advanced solid tumors[1].
In Vitro
TNO155 shows an IC50 of 0.008 µM in KYSE520 pERK assay and shows an IC50 of 0.100 µM in KYSE520 5-day cell proliferation assay. The off-target IC50 values are 18 µM, 6.9 µM, and 11 µM for Cav1.2, VMAT, and SST3, respectively[1].
In Vivo
The oral bioavailability in mouse, rat and money are 78%, 86%, and 60%, respectively[1].
References & source
[1]. TNO155: SHP2 inhibitor
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.