MBC-11

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MBC-11 

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

MBC-11 Chemical Structure

CAS No. : 332863-86-2

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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[1].

体外研究
(In Vitro)

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell 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.

体内研究
(In Vivo)

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[1].
Weight gained in mice treated with up to 500 μg/day of MBC-11 is similar to the PBS treated group[1].
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)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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)[1].
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)[1].
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.

Clinical Trial

分子量

511.21

Formula

C11H20N3O14P3
CAS 号

332863-86-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Reinholz MM, et al. A promising approach for treatment of tumor-induced bone diseases: utilizing bisphosphonate derivatives of nucleoside antimetabolites. Bone. 2010 Jul;47(1):12-22.

    [2]. Zinnen SP, et al. First-in-Human Phase I Study of MBC-11, a Novel Bone-Targeted Cytarabine-Etidronate Conjugate in Patients with Cancer-Induced Bone Disease. Oncologist. 2019 Mar;24(3):303-e102.

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