产品描述
MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). It also has the potential to treat tumor-induced bone disease (TIBD).
体外活性
MBC-11 reduces KAS-6/1 cell growth from approximately 56% at 10-8 M to 6% at 10-5 M. MBC-11 displays similar activity profiles and obviously suppresses the growth of all three cell lines between 10-8 and 10-4 M [1].
体内活性
MBC-11 obviously reduces bone tumor burden compared to PBS- or zoledronate-treated mice. MBC-11 (0.04 μg/day, s.c.) has a lower incidence of bone metastases of 40% compared to those treated with PBS (90%) or 0.04 μg/day zoledronate (100%). Weight gained in mice treated with up to 500 μg/day of MBC-11 is similar to the PBS treated group. These results show that MBC-11 decreases bone tumor burden maintains the bone structure, and may increase overall survival, warranting further investigation as a treatment for tumor-induced bone disease (TIBD)[1].
Cas No.
332863-86-2
分子式
C11H20N3O14P3
分子量
511.21
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years