标签归档：triethylamine

MBC-11 triethylamine

发表于由

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 triethylamine 

MBC-11 triethylamine 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 triethylamine 具有用于肿瘤性骨病 (TIBD) 的潜力。

MBC-11 triethylamine

MBC-11 triethylamine Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

MBC-11 triethylamine is a first-in-class conjugate of the bone-targeting bisphosphonate etidronate covalently linked to the antimetabolite cytarabine (araC). MBC-11 triethylamine 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]

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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: 47% of 17 mice treated with MBC-11 had detectable bone metastases. 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

612.40

Formula

C17H35N4O14P3
运输条件

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

-20°C, sealed storage, away from moisture

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务