Gandotinib

Gandotinib, also known as LY2784544, is a potent and selective JAK inhibitor. LY2784544 in vitro selectivity for JAK2 was found to be equal or superior to known JAK2 inhibitors. LY2784544 effectively inhibited JAK2V617F-driven signaling and cell proliferation in Ba/F3 cells (IC50=20 and 55 nM, respectively). In vivo, LY2784544 effectively inhibited STAT5 phosphorylation in Ba/F3-JAK2V617F-GFP ascitic tumor cells (TED50=12.7 mg/kg) and significantly reduced (P<0.05) Ba/F3-JAK2V617F-GFP tumor burden in the JAK2V617F-induced MPN model (TED50=13.7 mg/kg, twice daily).

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CAT#R1971
CAS1229236-86-5
Synonyms/AliasLY2784544; LY 2784544; LY-2784544
Chemical Name3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(morpholin-4-ylmethyl)imidazo[1,2-b]pyridazin-6-amine
M.F/FormulaC23H25ClFN7O
M.W/Mr.469.9
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