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CAS No. : 1416241-23-0
MCE 国际站:Vamotinib
产品活性:Vamotinib (PF-114) 是一种有效的,选择性具有口服活性的酪氨酸激酶抑制剂。Vamotinib 抑制 BCR/ABL 和 BCR/ABL-T315I 的自磷酸化。Vamotinib 诱导细胞凋亡 (apoptosis)。Vamotinib 显示出抗增殖和抗肿瘤活性。Vamotinib 在耐药性费城染色体阳性 (Ph+) 白血病的研究中具有潜力。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:Bcr-Abl
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.
Vamotinib (0-1000 nM) inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I in a dose-dependent manner.
Vamotinib (0-2000 nM) shows anti-proliferative activity in Ba/F3 cells expressing native BCR/ABL.
Vamotinib (0-100 nM) induces apoptosis in Ba/F3 cells expressing BCR/ABL and BCR/ABL-T315I.
Vamotinib (0-1000 nM) inhibits the growth of Ph+ patient-derived cell lines in k562, kcl-22, SupB15, Tom-1, BV-173 cells.
Vamotinib (0-1000 nM) suppresses growth of Ph+ PD-LTC with nonmutational resistance as well as T315I mutation.
In Vivo: Vamotinib (25, 40 mg/kg; i.g.; daily for 14 consecutive days) shows anti-tumor activity.
Vamotinib (50 mg/kg; p.o.; once daily for 20 days) prolongs the survival of mice with both BCR/ABL- and BCR/ABL-T315I-driven CML-like disease.
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