MBC-11

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MBC-11 是首创的、骨靶向双膦酸乙酯与抗代谢物阿糖胞苷 (araC) 共价结合的偶联物。MBC-11 具有用于肿瘤性骨病 (TIBD) 的潜力。

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.

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.Cell Proliferation AssayCell Line:Human multiple myeloma cell lines (KAS-6/1, DP-6, KP-6).Concentration:Between 10-8 and 10-4 M.Incubation Time:48 hours.Result:Significantly inhibited multiple myeloma cell proliferation of each cell line at the majority of the tested concentrations.

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.

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332863-86-2

511.21

C11H20N3O14P3

>98% (HPLC)

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O[C@@H]1[C@@H](O[C@H](COP(OP(C(P(=O)(O)O)(C)O)(=O)O)(=O)O)[C@H]1O)N2C(=O)N=C(N)C=C2

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(-20℃)

With Ice Pack

≥ 2 years