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。

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.

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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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. Mian AA,et al. PF-114, a potent and selective inhibitor of native and mutated BCR/ABL is active against Philadelphia chromosome-positive (Ph+) leukemias harboring the T315I mutation. Leukemia. 2015 May;29(5):1104-14.
[2]. Ivanova ES, et al. PF?114, a novel selective inhibitor of BCR?ABL tyrosine kinase, is a potent inducer of apoptosis in chronic myelogenous leukemia cells. Int J Oncol. 2019 Jul;55(1):289-297.

In Vitro: DMSO : 50 mg/mL (93.89 mM; Need ultrasonic)配制储备液