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MBC-11 

目录号: HY-107093
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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.
Storage

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

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

Shipping

Room temperature in continental US; may vary elsewhere

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产品名称:
MBC-11
目录号:
HY-107093
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MBC-11

Cat. No.: HY-107093