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332863-86-2

中文名稱(chēng) 2(1H)-Pyrimidinone, 4-amino-1-[5-O-(1,3,4,5,5-pentahydroxy-4-methyl-1,3,5-trioxido-2-oxa-1,3,5-triphosphapent-1-yl)-β-D-arabinofuranosyl]-
英文名稱(chēng) 2(1H)-Pyrimidinone, 4-amino-1-[5-O-(1,3,4,5,5-pentahydroxy-4-methyl-1,3,5-trioxido-2-oxa-1,3,5-triphosphapent-1-yl)-β-D-arabinofuranosyl]-
CAS 332863-86-2
分子式 C11H20N3O14P3
分子量 511.21
MOL 文件 332863-86-2.mol
332863-86-2 結(jié)構(gòu)式 332863-86-2 結(jié)構(gòu)式

基本信息

中文別名
化合物 MBC-11
化合物 T11956L
英文別名
MBC-11
MBC 11,MBC11
2(1H)-Pyrimidinone, 4-amino-1-[5-O-(1,3,4,5,5-pentahydroxy-4-methyl-1,3,5-trioxido-2-oxa-1,3,5-triphosphapent-1-yl)-β-D-arabinofuranosyl]-

物理化學(xué)性質(zhì)

沸點(diǎn)880.1±75.0 °C(Predicted)
密度2.32±0.1 g/cm3(Predicted)
酸度系數(shù)(pKa)1.14±0.50(Predicted)

常見(jiàn)問(wèn)題列表

生物活性
MBC-11 是首創(chuàng)的、骨靶向雙膦酸乙酯與抗代謝物阿糖胞苷 (araC) 共價(jià)結(jié)合的偶聯(lián)物。MBC-11 具有用于腫瘤性骨病 (TIBD) 的潛力。
體外研究

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 Assay

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.
體內(nèi)研究

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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