TNO155

TNO155 is an orally bioavailable allosteric inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC₅₀ = 0.011 µM).¹ It is selective for SHP-2 over a panel of 52 kinases and phosphatases (IC₅₀s = >10 µM for all). TNO155 decreases phosphorylation of ERK in, and inhibits proliferation of, KYSE-520 human esophageal cancer cells (IC₅₀s = 0.011 and 0.1 µM, respectively). It acts synergistically with dabrafenib (Item No. 16989) and trametinib (Item No. 16292) to inhibit proliferation of B-RAF^V600E-expressing HT-29, RKO, and MDST8 colorectal cancer cells.² TNO155 (2.5, 10, and 20 mg/kg twice per day) reduces tumor growth in a KYSE-520 mouse xenograft model.¹

WARNING This product is not for human or veterinary use.

1. LaMarche, M.J., Acker, M., Argintaru, A., et al. Identification of TNO155, an allosteric SHP2 inhibitor for the treatment of cancer. J. Med. Chem. 63(22), 13578-13594 (2020).

2. Liu, C., Lu, H., Wang, H., et al. Combinations with allosteric SHP2 inhibitor TNO155 to block receptor tyrosine kinase signaling. Clin. Cancer Res. 27(1), 342-354 (2021).