产品
编 号:F323401
分子式:C11H20N3O14P3
分子量:511.21
产品类型
结构图
CAS No: 332863-86-2
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产品详情
生物活性:
MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 has the potential for tumor-induced bone disease (TIBD) research.
体内研究:
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%). MBC-11 also significantly decreases bone tumor burden compared to PBS- or zoledronate-treated mice. Weight gained in mice treated with up to 500 μg/day of MBC-11 is similar to the PBS treated group. These results demonstrate that MBC-11 decreases bone tumor burden, maintains bone structure, and may increase overall survival, warranting further investigation as a treatment for tumor-induced bone disease (TIBD).Animal Model:Approximately four-week old female Balb/c mice inoculated (s.c. injection into their mammary fatpads) with 500,000 4T1/luc cells at day 0 (breast tumor model).
Dosage:0.04, 0.4, or 4.0 μg/day.
Administration:S.C. daily from day 7 to 21.
Result:The dose of 0.04 μg/day had a lower incidence of bone metastases compared to those treated with PBS or 0.04 μg/day zoledronate.
Animal Model:Female Balb/c and SCID mice (four-six weeks old).
Dosage:500, 100, 1, or 0.01 μg/100 μL.
Administration:S.C. daily for 24 or 49 days.
Result:Weight gained in MBC-11 treated mice with different doses was similar to the PBS treated group.
体外研究:
MBC-11 shows similar activity profiles and significantly inhibits growth of all three cell lines between 10-8 and 10-4 M. MBC-11 decreases KAS-6/1 cell growth from approximately 56% at 10-8 M to 6% at 10-5 M.