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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]-

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]-, 332863-86-2, 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]-
CAS号:
332863-86-2
英文名:
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]-
英文别名:
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]-
中文名:
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]-
中文别名:
化合物 T11956L
CBNumber:
CB65891119
分子式:
C11H20N3O14P3
分子量:
511.21
MOL File:
332863-86-2.mol

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]-化学性质

沸点:
880.1±75.0 °C(Predicted)
密度:
2.32±0.1 g/cm3(Predicted)
酸度系数(pKa):
1.14±0.50(Predicted)
安全信息

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、用途与生产工艺

生物活性

MBC-11 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 具有用于肿瘤性骨病 (TIBD) 的潜力。

体外研究

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.

体内研究

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.

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]- 上下游产品信息

上游原料

下游产品


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]- 生产厂家

供应商联系电话电子邮件国家产品数优势度
TargetMol Chemicals Inc. +1-781-999-5354 +1-00000000000 marketing@targetmol.com 美国 19892 58
天津普西唐生物医药科技有限公司 010-60605840 psaitong@jm-bio.com 中国 29778 58
TargetMol中国(陶术生物) 4008200310 marketing@tsbiochem.com 中国 24017 58
苏州美石生物科技有限公司 1173954148q meishipharma@126.com 中国 20035 58
 

332863-86-2, 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]- 相关搜索:

  • C11H20N3O14P3
  • 化合物 T11956L
  • 332863-86-2
  • MBC 11,MBC11
  • MBC-11
  • 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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