Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis . Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia. Vamotinib inhibits ABL series kinases with IC 50 s of 0.49 nM (ABL), 0.78 nM (ABL T315I ), 9.5 nM (ABL E255K ), 2.0 nM (ABL F317I ), 7.4 nM (ABL G250E ), 1.0 nM (ABL H396P ), 2.8 nM (ABL M351T ), 12 nM (ABL Q252H ), and 4.1 nM (ABL Y253F ), respectively. Vamotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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