In Vitro |
Vamotinib (0-1 µM) inhibits ABL kinase and its mutants with IC50s of 0.49, 0.78, 1.0 µM for ABL, ABL(T315l), ABL(H396P), respectively[1]. Vamotinib (0-1000 nM) inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner[1]. Vamotinib (0-2000 nM) shows anti-proliferative activity in Ba/F3 cells expressing native BCR/ABL[1]. Vamotinib (0-100 nM) induces apoptosis in Ba/F3 cells expressing BCR/ABL and BCR/ABL-T315I[1]. Vamotinib (0-1000 nM) inhibits the growth of Ph+ patient-derived cell lines in k562, kcl-22, SupB15, Tom-1, BV-173 cells[1]. Vamotinib (0-1000 nM) suppresses growth of Ph+ PD-LTC with nonmutational resistance as well as T315I mutation[1]. Western Blot Analysis[1] Cell Line: Ba/F3 cells Concentration: 0, 10, 25, 50, 100, 500, 1000 nM Incubation Time: Result: Inhibited the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner and inhibited substrate phosphorylation as shown by the reduced Crkl-phosphorylation and downstream activation of Stat5 by BCR/ABL, as well as by BCR/ABL-T315I. Cell Proliferation Assay[1] Cell Line: Ba/F3 cells Concentration: 0, 50, 500, 2000 nM Incubation Time: Result: Potently inhibited proliferation of Ba/F3 cells expressing native BCR/ABL in a dose-dependent manner and shows no effects on empty vector-transduced Ba/F3 cells in the presence of IL-3 (10 ng/ml). Apoptosis Analysis[1] Cell Line: Ba/F3 cells Concentration: 0-100 nM Incubation Time: Result: Induced apoptosis in Ba/F3 cells expressing BCR/ABL and BCR/ABL-T315I in a dose dependent manner.
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