Formulation: A solid
Formal Name: (7S)-3-amino-14-ethyl-11-fluoro-4,5,6,7,13,14-hexahydro-7-methyl-4-oxo-1,15-etheno-1H-pyrazolo[4,3-f][1,4,8,10]benzoxatriazacyclotridecine-12-carbonitrile
Purity: ≥98%
Formula Markup: C20H20FN7O2
Formula Weight: 409,4
Shelf life (days): 1460
CAS Number: 2271119-26-5
Notes: TPX-0022 is an inhibitor of Src, MET, and CSF-1 receptor tyrosine kinase (FMS) kinases (IC50s = 0.12, 0.14, and 0.76 nM, respectively).{67128} It inhibits the proliferation of MKN45 and SNU-5 human gastric cancer cells (IC50s = 0.2 and 0.17 nM, respectively), as well as Ba/F3 pro-B cells expressing TEL-CSF1R (IC50 = 19.3 nM). TPX-0022 (100 nM) inhibits cell migration of HCC827 human lung cancer cells. It inhibits tumor growth in an MKN45 mouse xenograft model when administered at doses of 10 and 30 mg/kg. TPX-0022 (10 mg/kg) also inhibits phosphorylation of MET at Tyr1234 and Tyr1349 in the same model.
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