Formulation: A solid
Formal Name: N-[6-[[6-(4-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazin-3-yl]thio]-2-benzothiazolyl]-N′-[2-(4-morpholinyl)ethyl]-urea
Purity: ≥98%
Formula Markup: C25H23FN8O2S2
Formula Weight: 550,6
Shelf life (days): 1460
CAS Number: 1116743-46-4
Notes: SAR125844 is an inhibitor of the receptor tyrosine kinase c-Met (IC50 = 4 nM).{65672} It is selective for c-Met over tropomyosin-related kinase A (TrkA), TrkB, PDGFRα, Axl, and Mer (IC50s = 39, 280, 55, 87, and 105 nM, respectively).{65671} SAR125844 inhibits the proliferation of MKN45 gastric cancer cells (IC50 = 7 nM).{65672} In vivo, SAR125844 (20 mg/kg) inhibits intratumoral c-Met phosphorylation in a MET-amplified Hs 746T gastric cancer mouse xenograft model. SAR125844 (10-45 mg/kg) also reduces tumor volume in Hs 746T and SNU-5 gastric cancer mouse xenograft models.{65671}
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