Description
KX2-391 can inhibit Src with IC50 of 72 nM.
Storage
2 years at -20 centigrade
Molecular Formula
C26H29N3O3
Chemical Name
N-benzyl-2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)acetamide
Solubility
DSMO 86 mg/mL Water
In vitro
As a small molecule and non-ATP competitive inhibitor, KX2-391 can inhibit Src tyrosine kinase signaling inhibitor with an IC50 of 72 nM by targeting the substrate binding pocket of Src. KX2-391 can also inhibit tubulin polymerization. For cell lines KX2-391 can inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation.
In vivo
In pre-clinical animal models of cancer, orally administered KX2-391 was shown to inhibit primary tumor growth and to suppress metastasis. In combination with certain chemotherapeutic agents, KX2-391 can reduce the doses of some current cytotoxic agents. KX2-391 is currently in Phase-2 testing for solid tumors.
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