Product Data Sheet

S116836

Catalog No. A30990

main product photo
S116836 is a potent BCR-ABL tyrosine kinase inhibitor that effectively targets both wild-type and T315I BCR-ABL variants. It induces apoptosis and arrests the cell cycle in the G0/G1 phase, promoting increased reactive oxygen species (ROS) and reduced glutathione (GSH) levels in BaF3/WT and BaF3/T315I cells. Additionally, S116836 inhibits SRC, LYN, HCK, LCK, BLK, as well as receptor tyrosine kinases including FLT3, TIE2, KIT, and PDGFR-β, demonstrating significant antitumor activity. This compound also features an alkyne group, making it suitable for click chemistry applications, particularly the copper-catalyzed azide-alkyne cycloaddition (CuAAc).
Chemical Information
Catalog NumA30990
M. Wt502.49
FormulaC27H21F3N6O
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.1257628-57-1
Synonyms
SMILESO=C(C1=CC=C(C(C#CC2=CN=C(N=C2)NC3CC3)=C1)C)NC4=CC(C(F)(F)F)=CC(N5C=CN=C5)=C4
Biological Activity
DescriptionS116836 is a potent BCR-ABL tyrosine kinase inhibitor that effectively targets both wild-type and T315I BCR-ABL variants. It induces apoptosis and arrests the cell cycle in the G0/G1 phase, promoting increased reactive oxygen species (ROS) and reduced glutathione (GSH) levels in BaF3/WT and BaF3/T315I cells. Additionally, S116836 inhibits SRC, LYN, HCK, LCK, BLK, as well as receptor tyrosine kinases including FLT3, TIE2, KIT, and PDGFR-β, demonstrating significant antitumor activity. This compound also features an alkyne group, making it suitable for click chemistry applications, particularly the copper-catalyzed azide-alkyne cycloaddition (CuAAc).
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