TNO155 is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2 /src homology region 2 domain phosphatase /PTPN11) with IC50 of 0.011 µM. TNO155 has potential antineoplastic activity.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Protein-tyrosine phosphatase 2C inhibitor
Product Description
Information
TNO155 TNO155 is an inhibitor of protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2 /src homology region 2 domain phosphatase /PTPN11) with IC50 of 0.011 µM. TNO155 has potential antineoplastic activity.
Targets
SHP-2 (Cell-free assay) 0.011 μM
In vitro
TNO155 inhibits KYSE520 pERK and KYSE520 5-day cell proliferation with IC50 of 0.008 µM and of 0.100 µM, respectively. The off-target IC50 are 18 µM, 6.9 µM, 11 µM and > 30μM for Cav1.2, VMAT, SST3 and all others, respectively.
In vivo
TNO155 is a potent and selective first-in-class inhibitor of wild-type SHP2, with high oral bioavailability and BCS class I properties. The oral bioavailability of TNO155 in mouse, rat and money are 78%, 86%, and 60%, respectively.
1.LaMarche MJ, Acker M, Argintaru A, Bauer D, Boisclair J, Chan H, Chen CH, Chen YN, Chen Z, Deng Z et al.. (2020) Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer.. J Med Chem, 63 (22):(13578-13594). [PMID:32910655]
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K2211741