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]-
| 中文名称 | 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]- |
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| 中文同义词 | 化合物 T11956L;化合物 MBC-11 |
| 英文名称 | 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]- |
| 英文同义词 | 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]-;MBC-11;MBC 11,MBC11 |
| CAS号 | 332863-86-2 |
| 分子式 | C11H20N3O14P3 |
| 分子量 | 511.21 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 332863-86-2.mol |
| 结构式 | ![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]- 结构式](CAS/20210305/GIF/332863-86-2.gif) |
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]- 性质
| 沸点 | 880.1±75.0 °C(Predicted) |
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| 密度 | 2.32±0.1 g/cm3(Predicted) |
| 酸度系数(pKa) | 1.14±0.50(Predicted) |
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]- 用途与合成方法
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. |
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. |