Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: (3S,4S)-8-[6-amino-5-[(2-amino-3-chloro-4-pyridinyl)thio]-2-pyrazinyl]-3-methyl-2-oxa-8-azaspiro[4.5]decan-4-amine
Purity: ≥98%
Formula Markup: C18H24ClN7OS
Formula Weight: 421.9
CAS Number: 1801765-04-7
Notes: TNO155 is an orally bioavailable allosteric inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = 0.011 µM).{61227} 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-RAFV600E-expressing HT-29, RKO, and MDST8 colorectal cancer cells.{61228} TNO155 (2.5, 10, and 20 mg/kg twice per day) reduces tumor growth in a KYSE-520 mouse xenograft model.{61227}