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MBC-11 

目录号: HY-107093
产品使用指南

MBC-11是一线的、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。具有治疗肿瘤性骨病 (TIBD) 的潜力。

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MBC-11 Chemical Structure

MBC-11 Chemical Structure

CAS No. : 332863-86-2

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Description

MBC-11 is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). Has potential to treat tumor-induced bone disease (TIBD)[1].

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].

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.
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].

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.
References
Molecular Weight

511.21

Formula

C₁₁H₂₀N₃O₁₄P₃

CAS No.

332863-86-2

SMILES

CC(P(O)(O)=O)(P(O)(OP(O)(OC[C@@H]1[C@@H](O)[C@H](O)[C@H](N2C=CC(N)=NC2=O)O1)=O)=O)O

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
MBC-11
目录号:
HY-107093
需求量:

MBC-11

Cat. No.: HY-107093